Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Ian B. Moses"'
Autor:
Ian B. Moses, Neal W. Sach, Loïc R E Pantaine, Andre Shavnya, David C. Blakemore, Xinlan A F Cook, Michael C. Willis
Publikováno v:
Angewandte Chemie (International Ed. in English)
Heteroaromatic sulfinates are effective nucleophilic reagents in Pd0‐catalyzed cross‐coupling reactions with aryl halides. However, metal sulfinate salts can be challenging to purify, solubilize in reaction media, and are not tolerant to multi‐
Autor:
Janette McKnight, Andre Shavnya, Neal W. Sach, David C. Blakemore, Ian B. Moses, Michael C. Willis
An efficient Pd-catalyzed one-pot desulfinative cross-coupling to access medicinally relevant di(hetero)arylmethanes is reported. The method is reductant-free, and involves a sulfinate transfer reagent and a Pd-catalyst mediating the union of two ele
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22e95feaf513ca29b2860e3f04451000
https://ora.ox.ac.uk/objects/uuid:5b1f7d51-3f8e-4d6d-8a88-c2c898529e93
https://ora.ox.ac.uk/objects/uuid:5b1f7d51-3f8e-4d6d-8a88-c2c898529e93
Publikováno v:
Organic Process Research & Development. 16:697-703
The development and implementation of a safe and scalable process for the manufacture of corticosteroid PF-4714224 (1) is described. Initial routes used to synthesise analogues from this series directly from fluocinolone acetonide (2) were unsuitable
Autor:
Alan John Pettman, Nieves Castro, Iain Robert Gladwell, Ian B. Moses, Natalie A. Morrison, Maninder S. Panesar, Nicholas Murray Thomson, Pieter D. de Koning
Publikováno v:
Organic Process Research & Development. 15:1256-1265
The development of a practical, scalable route to PF-00610355 (8) is described. In this convergent approach, amine 9 is coupled to protected bromohydrin 1 to give the doubly protected intermediate 26. TBS-Deprotection of 26 affords the benzyl protect
Autor:
Iain Robert Gladwell, Ian B. Moses, Nicholas Murray Thomson, Maninder S. Panesar, Alan John Pettman, Pieter D. de Koning
Publikováno v:
Organic Process Research & Development. 15:1247-1255
The initial route used to prepare PF-00610355 (8) for early clinical development is described. Through careful choice of solvent, an efficient, telescoped route to carboxylic acid 23 was developed, affording this late-stage intermediate in 80% yield
Autor:
Andrew J. Bibb, Petar I. Nikiforov, Stuart Field, Steven J. Fussell, Olivier Dirat, Mason Clive Philip, Alan John Pettman, Colin M. Burns, Green Stuart, Ian B. Moses, Jinu S. Mathew, Graham Checksfield, Barry Richard Dillon, Flavien Susanne, Suju Mathew
Publikováno v:
Organic Process Research & Development. 15:1010-1017
We report the discovery and optimization of an amine-promoted Friedel–Crafts alkylation of cinnamaldehyde with 4-hydroxymethyl phenol. This reaction has been used successfully on commercial scale (200 kg) in the context of the manufacture of fesote
Autor:
Ian B. Moses, Rick Rodriguez, Peter Robert Rose, Corey L. Stanchina, Cuthbertson Timothy J, Asayuki Kamatani, Pieter D. de Koning, Alison Sandoval, Kyle Kissick, Robert Moore, Leera Rahman, Douglas McAndrew, Armando Urbina, David C. Boyles
Publikováno v:
Organic Process Research & Development. 15:1018-1026
A robust six-step process for the synthesis of crizotinib, a novel c-Met/ALK inhibitor currently in phase III clinical trials, has been developed and used to deliver over 100 kg of API. The process includes a Mitsunobu reaction, a chemoselective redu
Autor:
Alan John Pettman, Daniel R. Yazbeck, Maninder S. Panesar, Nicholas Murray Thomson, Ian B. Moses, Iain Robert Gladwell, Pieter D. de Koning, Natalie A. Morrison
Publikováno v:
Organic Process Research & Development. 15:871-875
An efficient process to ethyl [3-(2-amino-2-methylpropyl)phenyl]acetate 6 has been developed. Key steps include a novel enzymatic desymmetrization of diester 2 and a Ritter reaction between alcohol...
Autor:
Ian B. Moses, M. Jonathan Fray, Adam T. Gillmore, Keith A. Reeves, Lisa R. Thompson, Melanie S. Glossop, David J. McManus, Céline F. B. Praquin
Publikováno v:
Organic Process Research & Development. 14:263-271
The development is described of a viable kilo-scale synthesis of the Nav1.8 sodium channel modulator, N-methyl-6-amino-5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide (PF-1247324) in five steps, starting from 6-amino-5-bromo-2-picoline, in 33% overal
Autor:
Pieter D. de Koning, Nieves Castro, Iain R. Gladwell, Natalie A. Morrison, Ian B. Moses, Maninder S. Panesar, Alan J. Pettman, Nicholas M. Thomson
Publikováno v:
Organic Process Research & Development; Nov2011, Vol. 15 Issue 6, p1256-1265, 10p