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Enantioselective microbial reduction of 6-oxo-8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione

Autor: Jianqing Li, Linda Chu, Venkata B. Nanduri, Atul S. Kotnis, William L. Parker, Richard H. Mueller, Ramesh N. Patel, Mark Liu

Publikováno v: Tetrahedron: Asymmetry. 16:2778-2783

The enantioselective microbial reduction of 6-oxo-8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione 1 to either of the corresponding (R)- or (S)-6-hydroxy-8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4c0ead0068215d5d10b0b70885eb1a3e
https://doi.org/10.1016/j.tetasy.2005.07.015

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Preparation of (R)- and (S)-6-hydroxybuspirone by enzymatic resolution or hydroxylation

Autor: Ronald L. Hanson, Ramesh N. Patel, William L. Parker, David B. Brzozowski, Atul S. Kotnis, Mark Liu, Thomas P. Tully

Publikováno v: Tetrahedron: Asymmetry. 16:2711-2716

6-Hydroxybuspirone is an active metabolite of the antianxiety drug buspirone. The (R)- and (S)-enantiomers of 6-hydroxybuspirone were prepared using an enzymatic resolution process. l -Amino acid acylase from Aspergillus melleus (Amano Acylase 30000)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9edda988653835448c5c905474ccf55e
https://doi.org/10.1016/j.tetasy.2005.07.020

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Development of a Safe and Scalable Oxidation Process for the Preparation of 6-Hydroxybuspirone: Application of In-Line Monitoring for Process Ruggedness and Product Quality

Autor: Eric D. Dowdy, Daniel J. Watson, and Simon Leung, B. C. O'reilly, Depue Jeffrey S, Atul S. Kotnis

Publikováno v: Organic Process Research & Development. 8:616-623

The development of a safe and scalable oxidation process for the hydroxylation of the azapirone psychotropic agent buspirone (1) to furnish 6-hydroxybuspirone (2) is described. A mechanistic understanding of how key process factors affected product q

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2e165cbef2fe13ab9a6cec45655514bc
https://doi.org/10.1021/op049918r

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A pilot-scale synthesis of (1R)-trans-2-(2,3-dihydro-4-benzofuranyl)cyclopropanecarboxylic acid: a practical application of asymmetric cyclopropanation using a styrene as a limiting reagent

Autor: Michael Totelben, Richard H. Mueller, Jollie D. Godfrey, James H. Simpson, Jason Hamm, Edward J. Delaney, Victor W. Rosso, Rajendra P. Deshpande, Atul S. Kotnis, Rita Fox, David J. Kacsur

Publikováno v: Tetrahedron: Asymmetry. 14:3569-3574

Asymmetric cyclopropanation of styrene 1 (as the limiting reagent) was demonstrated using excess ethyl diazoacetate and catalytic Ru(ip-Pybox). Selective hydrolysis of the resulting 90:10 trans : cis mixture of cyclopropane 4 generated cyclopropyl ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b6daf43781bfc4eec1ae829be10209c2
https://doi.org/10.1016/j.tetasy.2003.08.041

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Generation and Fate of Regioisomeric Side-Chain Impurities in the Preparation of Fosinopril Sodium

Autor: Atul S. Kotnis, Mary B. Gardineer, Maria L. Coradetti, Neal G. Anderson, John A. Cronin, Venkatapuram A. Palaniswamy, and David A. Lust, Merrill L. Davies

Publikováno v: Organic Process Research & Development. 1:315-319

A regioisomeric impurity is routinely formed during preparation of the first intermediate of the fosinopril sodium side chain. This first step, the radical-initiated condensation of 4-phenyl-1-butene (1) and aqueous hypophosphorous acid, provides low

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::706781a3d5c2f6e33b50569ca55929fb
https://doi.org/10.1021/op9702105

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Trifluoroacetic Acid-Mediated Cleavage of a Triethylsilyl Protecting Group: Application in the Final Step of the Semisynthetic Route to Paclitaxel (Taxol)

Autor: Mark Liu, Chenkou Wei, Dale Vanyo, Rachel Mathew, William J. Winter, F. Taha Comezoglu, Kumar Gadamsetti, Victor W. Rosso, Ciro J. Spagnuolo, Gerald L. Powers, Atul S. Kotnis, Raymond E. Weaver, Ambarish K. Singh, Bich D. Phan, David A. Lust, Merrill L. Davies, Kenneth S. Bembenek, Wen-Sen Li, Venkatapuram A. Palaniswamy

Publikováno v: Organic Process Research & Development. 7:25-27

The final step of the semisynthetic route to paclitaxel involves cleavage of the triethylsilyl (TES) protecting group from the C-7 hydroxyl group. Paclitaxel is an extremely complex molecule, and standard deprotection conditions led to formation of s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::56da05cea73431e136028ba13fc5eb42
https://doi.org/10.1021/op020221k

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Removal of Pinanol via Continuous Steam Distillation

Autor: Edward J. Delaney, Ambarish K. Singh, Donald C. Kientzler, San Kiang, J. Siva Prasad, Atul S. Kotnis, Dale Vanyo, Joseph Bush, Sushil K. Srivastava

Publikováno v: Organic Process Research & Development. 6:301-303

A practical procedure for the efficient removal of pinanol from the reaction mixture has been developed. The process was based on the observation that pinanol can be easily removed by steam distill...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a61e0bd8e0e36c7a4e1738e8044edec4
https://doi.org/10.1021/op010209c

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