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1 BIODATA Name: Dr. H. B. Borate Date of Birth: 1 st June 1957 Address: Division of Organic Chemistry, National Chemical Laboratory, Pashan Road, Pune Designation: Scientist F Educational Qualifications: Degree University Subject Year of Passing Division/ Class B. Sc. Shivaji University, Kolhapur, Chemistry 1978 First class India with distinction M. Sc. Shivaji University, Kolhapur, Organic Chemist 1980 First class India with distinction Ph. D. Pune University, Pune, India Chemistry 1986 Thesis Research Experience: * Working as a scientist at National Chemical Laboratory since 1980 * Research experience in synthetic organic chemistry including two years of postdoctoral fellowship at Southern Methodist University, Dallas, Texas, USA * Development of methodologies for organic reactions using heterogeneous catalysts * Synthesis of biologically active compounds and development of processes for drugs and drug-intermediates Publications : 45 Patents Filed : 23
2 List of papers published 1. A convenient approach to the total synthesis of (±)-4-demethoxydaunomycinone; A. V. Rama Rao, B. Chanda and H. B. Borate; Tetrahedron, 38 (24), 3555 (1982). 2. A regiospecific approach to the synthesis of (±)-7,9-dideoxydaunomycinone; A. V. Rama Rao, B. Chanda and H. B. Borate; Ind. J. Chem., 22B, 521 (1983). 3. A general synthesis of 11-deoxyanthracyclines; A. V. Rama Rao, B. Chanda and H. B. Borate; Syn. Commun., 14 (3), 257 (1984). 4. Synthesis of (±)-7,9-dideoxydaunomycinone; B. Chanda and H. B. Borate; Ind. J. Chem., 24B, 1002 (1985). 5. Asymmetric synthesis of R-(-)-2-acetyl-2-hydroxy-5-methoxy-1,2,3,4- tetrahydronaphthalene- A key synthon for the synthesis of 11-deoxyanthracyclinones; A. V. Rama Rao, B. Chanda, H. B. Borate and M. Gupta; Ind. J. Chem., 25B, 9 (1986). 6. The preparation of the first α-vinylidenepenams; J. D. Buynak, H. B. Borate, C. Husting, T. Hurd, J. Vallabh, J. Mathew, J. Lambert and U. Siriwardane; Tet. Lett., 29 (40), 5053 (1988). 7. The preparation and use of metallo-6-vinylidenepenams; J. D. Buynak, H. B. Borate, G. Lamb, H. Isom, C. Husting, and Dipti Khasnis; J. C. S. Chem. Commun., 294 (1990). 8. Synthesis of 6-vinylidenepenams; J. D. Buynak, H. B. Borate, G. Lamb, D. Khasnis, H. Isom, C. Husting and U. Siriwardane; JOC, 58 (6), 1325 (1993). 9. Monitoring the conversion of cycloheptanone to methyl 7-oxoheptanoate by gas chromatography; R. D. Wakharkar, S. S. Biswas, H. B. Borate and D. E. Ponde; J. Chromatography A, 662, 420 (1994).
3 10. Natural kaolinitic clay: a remarkable reusable solid catalyst for the selective protection of aldehydes and ketones; D. E. Ponde, H. B. Borate, A. Sudalai, T. Ravindranathan and V. H. Deshpande; Tet. Lett., 37 (26), 4605 (1996). 11. First total synthesis of ( + )-brasiliquinone-b; M. L. Patil, H. B. Borate, D. E. Ponde, B. M. Bhawal and V. H. Deshpande; Tet. Lett., 40 (23), 4437 (1999). 12. First total synthesis of the antitumor antibiotic (+)-resorthiomycin; D. E. Ponde, S. Ramalingam, M. L. Patil, H. B. Borate and V. H. Deshpande; Tet. Lett., 40 (29), 5399 (1999). 13. Some observations on tiaprost mediated induced spawning of goldfish Carassius auratus (Linnaeus); H. S. Jagtap, S. S. Ghumare, H. B. Borate, R. D. Wakharkar and T. Ravindranathan; Ind. J. Fish., 47 (4), 371 (2000). 14. Extraction of waterborne prostaglandins from female goldfish, Carassius auratus (Linnaeus); S. S. Ghumare, H. S. Jagtap, H. B. Borate, R. D. Wakharkar and T. Ravindranathan; Ind. J. Fish., 48 (3), 337 (2001). 15. Benzyl trimethylammonium hydroxide catalyzed nitroaldol condensation; V. J. Bulbule, H. B. Borate, R. Deshmukh and V. H. Deshpande; Syn. Commun., 31 (23), 3623 (2001). 16. Pheromonal activity of prosolvin in goldfish C. auratus; H. S. Jagtap, S. S. Ghumare, H. B. Borate, R. D. Wakharkar and T. Ravindranathan; J. Appl. Aquaculture, 11 (3), 81 (2001). 17. Quantitative assessment of milt in prostaglandin induced milters of Labeo rohita (Ham); S. S. Ghumare, H. S. Jagtap, H. B. Borate, R. D. Wakharkar, T. Ravindranathan, B. Mondal, S. Gupta and S. Rath; J. Aqua. Trop., 16 (2), 165 (2001). 18. Total synthesis of (+)-brasiliquinone-b; M. L. Patil, H. B. Borate, D. E. Ponde and V. H. Deshpande; Tetrahedron, 58, 6615 (2002). 19. Simple synthesis of two naphthoquinone antibiotics psychorubrin and pentalongin; V. J. Bulbule, P. S. Koranne, H. B. Borate and V. H. Deshpande; Syn. Commun., 33 (4), 587 (2003). 20. Microwave assisted solvent-free synthesis of dihydropyrimidinones by Biginelli reaction
4 over Si-MCM-41 supported FeCl 3 catalyst; V. R. Choudhary, V. H. Tillu, V. S. Narkhede, H. B. Borate and R. D. Wakharkar; Catalysis Commun., 4 (9), 449 (2003). 21. Synthetic studies towards the benzophenone precursor for balanol; M. L. Patil, V. H. Deshpande, S. Ramlingam and H. B. Borate; Tetrahedron, 60 (8), 1869 (2004). 22. Li-X-type zeolite mediated Michael addition of thiols to cyclic enones and its application in the synthesis of 13-thiaprostaglandins; P. D. Shinde, V. A. Mahajan, H. B. Borate, V. A. Tillu, R. Bal, A. Chandwadkar and R. D. Wakharkar; J. Mol. Cat. A: Chemical, 216 (1), 115 (2004). 23. Selective cleavage of 2,3-O-isopropylidene group: a case of anchimeric assistance from O-glycoside; R. D. Wakharkar, M. B. Sahasrabuddhe, H. B. Borate and M. K. Gurjar; Synthesis, (11), 1830 (2004). 24. Solvent free selective silylation of alcohols, phenols and naphthols with HMDS catalyzed by H-β zeolite; V. H. Tillu, V. H. Jadhav, H. B. Borate and R. D. Wakharkar; ARKIVOC, (xiv), 83 (2004). 25. Thioacetalization of the carbonyl function, transthioacetalization of acetals, ketals, oximes and hydrazones catalysed by aqueous hydrobromic acid; P. D. Shinde, H. B. Borate and R. D. Wakharkar; ARKIVOC, (xiv), 110 (2004). 26. Convenient synthesis of 5-methylene-4-substituted-2(5H)-furanones; V. A. Mahajan, P. D. Shinde, H. B. Borate and R. D. Wakharkar; Tet. Lett., 46 (6), 1009 (2005). 27. Microwave promoted solvent-free one-pot synthesis of N,N -disubstituted urea derivatives; V. H. Jadhav, S. S. Deshpande, H. B. Borate and R. D. Wakharkar; J. Chem. Res., (3), 205 (2005). 28. The synthesis of substituted tetrahydro-1h-xanthen-1-ones and xanthenes; M. L. Patil and H. B. Borate; J. Chem. Res., 454 (2005). 29. A simple method for deprotection of tert-butyldimethylsilyl ethers by using stannous chloride under microwave irradiation; V. H. Jadhav, H. B. Borate and R. D. Wakharkar; Ind. J. Chem., 45B, 322 (2006).
5 30. Efficient synthesis of 1,4-dihydronaphthalenelignans from 5-methylene-4- substituted- 2(5H)-furanones and a concise synthesis of solafuranone; V. A. Mahajan, H. B. Borate and R. D. Wakharkar; Tetrahedron, 62, 1258 (2006). 31. Efficient N-arylation of amines catalyzed by Cu-Fe-hydrotalcite; V. H. Jadhav, D. K. Dumbre, V. B. Phapale, H. B. Borate and R. D. Wakharkar; Cat. Commun. 8, 65 (2007). 32. Simple and efficient synthesis of thysanone methyl ether; V. J. Bulbule, P. S. Koranne, V. H. Deshpande and H. B. Borate; Tetrahedron, 63 (1), (2007). 33. Enantiomeric separation of novel anticancer agent 5-hydroxy-3-(4-methoxyphenyl)-2- (3,4,5- trimethoxyphenyl)-cyclopent-2-en-1-one; Popat D. Shinde, Vinod H. Jadhav, Hanumant B. Borate, Sunil R. Bhide, Kiran B. Sonawane and Radhika D. Wakharkar; J. Chromatography A, 1138, (2007). 34. Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis- restricted analogues of combretastatin A-4 as novel anticancer agents; M. K. Gurjar, R. D. Wakharkar, A. T. Singh, M. Jaggi, H. B. Borate, P. D. Shinde, R. Verma, R. Praveen, S. Dutt, G. Singh, V. Sanna, M. K. Singh, S. K. Srivastava, V. A. Mahajan, V. H. Jadhav, K. Dutta, K. Karthik, S. K. Agarwal, R. M. Mukherjee and A. C. Burman; J. Med. Chem. 50, (2007). 35. Oxidation of benzylic alcohols and sulfides over LaCoO 3 and TBHP; M. L. Patil, S. R. Maujan, H. B. Borate and B. S. Uphade; ARKIVOC, (i), 1-6 (2007). 36. One-step preparation of α-chlorostyrenes; H. B. Borate, A. G. Gaikwad, S. R. Maujan, S. P. Sawargave and K. M. Kalal; Tet. Lett. 48 (28), (2007). 37. Transesterification of α-haloesters and β- ketoesters over Mg-Al-hydrotalcites (HT)-like anionic clays; V. J. Bulbule, H. B. Borate, Y. S. Munot, V. H. Deshpande, S. P. Sawargave and A. G. Gaikwad; J. Mol. Cat. A: Chemical 276, (2007). 38. Facile synthesis of substituted styrenes and stilbenes mediated by palladium on zirconia; H. B. Borate, D. K. Dumbre, R. D. Wakharkar and V. R. Choudhary; J. Chem. Res., (2008). 39. A short synthesis of 3,6-disubstituted N-2-thienyl/aryl-indoles; H. B. Borate, S. P. Sawargave, S. R. Maujan;
6 Tetrahedron Lett. 50 (47), (2009). 40. Fluconazole analogues containing 2H-1,4-benzothiazin-3(4H)-one or 2H-1,4- benzoxazin-3(4h)-one moieties, a novel class of anti-candida agents; H. B. Borate, S. R. Maujan, S. P. Sawargave, M. A. Chandavarkar, S. R. Vaiude, V. A. Joshi, R. D. Wakharkar, R. Iyer, R. G. Kelkar, S. P. Chavan and S. S. Kunte; Bioorg. Med. Chem. Lett. 20 (2), (2010). 41. Novel hybrids of fluconazole and furanones: Design, synthesis and antifungal activity; H. B. Borate, S. P. Sawargave, S. P. Chavan, M. A. Chandavarkar, R. Iyer, A. C. Tawte, D. D. Rao, J. V. Deore, A. S. Kudale, P. S. Mahajan, G. S. Kangire; Bioorg. Med. Chem. Lett. 21 (16), (2011). 42. One-step synthesis of 4-alkyl-3-aryl-2,6-dicyanoanilines and their use in the synthesis of highly functionalized 2,3,5,6,7- and 2,3,4,5,7-substituted indoles; Sangmeshwer P. Sawargave, Ananada S. Kudale, Jaydeep V. Deore, Dattatry S. Bhosale, Jaisingh M. Divse, Subhash P. Chavan and Hanumant B. Borate; Tetrahedron Lett. 52 (42), (2011). 43. Solvent-free one-pot synthesis of sulfonephthaleins from saccharin and phenols; V. H. Tillu, D. K. Dumbre, H. B. Borate, R. D. Wakharkar and V. R. Choudhary; Syn. Commun., 42 (8), (2012). 44. Synthesis of substituted 2,6-dicyanoanilines and related compounds. A review; H. B. Borate, A. S. Kudale and S. Agalave; Org. Prep. Proced. Int. 44 (6), (2012). 45. One-step method for the synthesis of aryl olefins from aryl aldehydes and aliphatic aldehydes; H. B. Borate, S. H. Gaikwad, A. S. Kudale, S. P. Chavan, S. G. Pharande, V. D. Wagh and V. S. Sawant; Tetrahedron Lett. 54 (12), (2013). List of patents filed 1. A new process for the synthesis of (±)-4-demethoxy-7-deoxydaunomycinone- A key intermediate for the manufacture of 4-demethoxydaunomycin, an antitumor compound; A. V. Rama Rao, B. Chanda and H. B. Borate; Ind. Patent Appl. No. 668/DEL/82 (1982). 2. An improved process for the preparation of silyl ethers; The intermediates for
7 prostaglandin synthesis; T. Ravindranathan, R. D. Wakharkar and H. B. Borate; Ind. Patent Appl. No. 1954/DEL/96 (1996). 3. An improved process for the preparation of substituted 2-oxindole-1-carboxamides; T. Ravindranathan, R. D. Wakharkar, A. B. Sahasrabudhe, V. R. Kulkarni, V. H. Deshpande and H. B. Borate; Ind. Patent Appl. No. 2633/DEL/96 (1996). 4. A new process for the preparation of 5,6-didehydroprostaglandin analogues; T. Ravindranathan, R. D. Wakharkar and H. B. Borate; Ind. Patent Appl. No. 2736/DEL/96 (1996). 5. An improved process for the preparation of misoprostol; T. Ravindranathan, R. D. Wakharkar and H. B. Borate; Ind. Patent Appl. No. 2508/DEL/96 (1996). 6. A process for the preparation of (1R, cis)-(-)-caronaldehydic acid hemiacetal; T. Ravindranathan, S. V. Hiremath, A. B. Sahasrabudhe, V. R. Kulkarni, and H. B. Borate; Ind. Patent Appl. No. 10/97(1997). 7. A process for the preparation of 3-sulfanyl cyclic ketones; T. Ravindranathan, R. D. Wakharkar, H. B. Borate, P. D. Shinde, S. S. Ghumare and H. S. Jagtap; Ind. Patent Appl. No. NF 374/99 (1999). 8. Novel 3-sulfanyl cyclic ketones T. Ravindranathan, R. D. Wakharkar, H. B. Borate, P. D. Shinde, V. A. Mahajan, S. S. Ghumare and H. S. Jagtap Indian Patent Appl. No. NF 80/2000 (2000). 9. A process for the preparation of optically active alkyl 4-phenyl-2-[(trifluoroacetyl)amino] butanoate; M. K. Gurjar, R. D. Wakharkar, H. B. Borate and P. A. Waske; Ind. Patent Appl. No. 99/DEL/2001 (2001) 10. A process for the preparation of 2-aryl-4-hydroxy-cyclopent-2-en-1-ones; M. K. Gurjar, R. D. Wakharkar, H. B. Borate, P. D. Shinde, V. A. Mahajan, V. H. Jadhav and A. M. Wagh; Ind. Patent Appl. No. NCL (2002). 11. A process for the preparation of 2,3-diaryl-4-(tert-butyldimethylsilyloxy)cyclopent-2-en- 1-one; M. K. Gurjar, R. D. Wakharkar, H. B. Borate, P. D. Shinde, V. A. Mahajan, V. H. Jadhav and A. M. Wagh;
8 Ind. Patent Appl. No. NCL (2002). 12. A process for the preparation of 5-methylene-4-benzyl(substituted)-2(5H)-furanone; M. K. Gurjar, R. D. Wakharkar, H. B. Borate, P. D. Shinde, V. A. Mahajan and M. H. Bhure; Ind. Patent Appl. No. NCL (2002). 13. Preparation of cyclopent-2-en-1-ones as antitumor agents; M. K. Gurjar, R. D. Wakharkar, G. R. Desiraju, A. Nangia, J. S. Yadav, A. C. Burman, R. Mukherjee, H. B. Borate, S. Chandrasekhar, M. Jaggi, A. T. Singh, K. K. Kapoor, S. Sarkhel and K. V. V. M. Sairam; US Patent Appl. No (2003). 14. A novel 2,3-diaryl-5-tert-butyldimethylsilyloxycyclopent-2-en-1-one and the process for the preparation thereof; M. K. Gurjar, R. D. Wakharkar, H. B. Borate, P. D. Shinde, V. A. Mahajan, V. H. Jadhav, A. M. Wagh, S. S. Deshpande, M. V. Deshmukh, G. J. Mhaske, N. D. Yadav and M. H. Bhure; Ind. Patent Appl. No. 0723/DEL/2005 (2005). Filing date: March 31, 2005; Publication date: November 10, Compounds with antifungal properties and process thereof; M. K. Gurjar, R. D. Wakharkar, H. B. Borate, R. G. Kelkar, A. Murugan, M. A. Chandavarkar, S. V. Joshi and S.R. Vaiude US Patent Applied; Appl. Serial No. 11/498,805 (2006); US 2007/ A-1; Nov 8, 2007 Indian Patent no: ; Application no: 713/MUM/2006; Date of filing: 08/05/2006; Date of grant: 09/09/ Thieno-[2,3-d]pyrimidin-4(3H)-one compounds with antifungal properties and process thereof; H. B. Borate, S. R. Maujan, S. P. Sawargave, M. A. Chandavarkar, S. V. Joshi and S. R. Vaiude; Ind Patent Applied; Appl. No. 438/MUM/2008 ( ); PCT International Application No. PCT/IN08/ dated 05/09/ Thiophene containing analogues of fluconazole as antifungal agents and process thereof; H. B. Borate, S. P. Sawargave, S. R. Maujan, M. A. Chandavarkar, S. R. Vaiude and V. A. Joshi; Ind Patent Applied; Appl. No. 1595/MUM/2007 ( ); US pat appl. 2132/MUM/2008 dt Antifungal compounds containing benzothiazinone, benzoxazinone or benzoxazolinone and process thereof ; H. B. Borate, S. R. Maujan, S. P. Sawargave, R. G. Kelkar, R. D. Wakharkar, M. A. Chandavarkar, S. R. Vaiude and V. A. Joshi;
9 Ind Patent Applied; Appl. No. 2306/MUM/2008 ( ) 19. Enantiomers of fluconazole analogues containing thieno-[2,3-d]pyrimidin-4(3h)-one moiety as antifungal agents; H. B. Borate, S. R. Maujan, S. P. Sawargave, S. P. Chavan, M. A. Chandavarkar, R. Iyer, V. Nawathye, G. Chavan. A. Tawte; Ind Patent Applied; Appl. No. 735/MUM/2011 ( ); Invention Disclosure No. INV ; PCT/IN2011/ ( ). 20. Hybrid molecules containing pharmacophores of fluconazole as antifungal agents and their preparation; H. B. Borate, S. P. Sawargave, S. P. Chavan, M. A. Chandavarkar, R. Iyer, A. C. Tawte, D. D. Rao; Ind Patent Applied; Appl. No. 1750/MUM/2011 ( ); Invention Disclosure No. INV Optically active fluconazole analogues containing thiophenes as antifungal agents H. B. Borate, S. P. Sawargave, S. P. Chavan, M. A. Chandavarkar, R. Iyer, A. C. Tawte, D. D. Rao; Ind Patent Applied; Appl. No. 3063/MUM/2011 ( ); Invention Disclosure No. INV Preparation of aryl olefins by reaction of aryl aldehyde and alkyl aldehyde H. B. Borate, S. H. Gaikwad, A. S. Kudale, S. P. Chavan, S. G. Pharande, V. D. Wagh, V. S. Sawant; Ind. Patent Provisional Filing Number: 3486/DEL/2012 Provisional filing date: Substituted, 4-(substituted phenoxymethyl)-1,2,3-triazole compounds with antifungal properties and methods for preparation thereof H. B. Borate, A. S. Kudale, S. P. Chavan, S. S. Kunte, M. A. Chandavarkar, R. Iyer, A. C. Tawte, D. D. Rao; Ind Patent Applied; Appl. No. 626/MUM/2013 (Filed on )
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