Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Pieter D. de Koning"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0e1470e98fe2368ffa01e135a9a795b4
https://doi.org/10.1021/op2002408
https://doi.org/10.1021/op2002408
Publikováno v:
Future Medicinal Chemistry. 3:1679-1701
The administration of compounds by a dry-powder inhaler presents significant challenges to the development and discovery chemist, owing to the stringent requirements placed upon the physical characteristics of the active pharmaceutical ingredient and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fd38e06c247f817054042ed2ce5334e
https://doi.org/10.4155/fmc.11.125
https://doi.org/10.4155/fmc.11.125
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ef178697153d9bcbc018eee494d246fc
https://doi.org/10.1021/op2001904
https://doi.org/10.1021/op2001904
Autor:
Lawson Jon P, Sastry A. Kunda, Pieter D. de Koning, Richard Vonder Embse, Lorraine Murtagh, Wei Kong
Publikováno v:
Organic Process Research & Development. 15:1046-1051
A convergent six-step process for the synthesis of PF-04191834 (1), a potent and selective 5-lipoxygenase inhibitor, has been developed and used to deliver over 20 kg of API. The process uses the same bond-forming steps as the initial medicinal chemi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9e1a86bf07d5365e9cb0fbf8d6d9aa68
https://doi.org/10.1021/op200173g
https://doi.org/10.1021/op200173g
Publikováno v:
Organic Process Research & Development. 15:1081-1084
When the process to prepare nonsteroidal progesterone receptor antagonist 5 was scaled up, significant problems were encountered, and as a result lower than expected yields were obtained. In particular, the alkylation of pyrazole 2 with chloromethyl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dbfc75caf3bf613f486f621a827c3b92
https://doi.org/10.1021/op200145j
https://doi.org/10.1021/op200145j
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6fd5a1469f77db90ff994ded3cb5273e
https://doi.org/10.1021/op200131n
https://doi.org/10.1021/op200131n
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...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::eae29c37bee97d64db0912c91bafab7b
https://doi.org/10.1021/op200108k
https://doi.org/10.1021/op200108k
Publikováno v:
Organic Process Research & Development. 15:1124-1129
An improved, simpler and potentially more economical route to (S)-N-Boc-2,6-dimethyltyrosine 1, based on a previously published route, is presented. Key modifications were to prepare the dehydroaminoacid hydrogenation substrate 6 in a one-pot process
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d7abac41717ed6a7fa0187785bde2e92
https://doi.org/10.1021/op200065p
https://doi.org/10.1021/op200065p
Autor:
Karl Richard Gibson, Yann C. Lecouturier, Paul A. Bradley, Malcolm C. Mackenny, Toby J. Underwood, Cedric Poinsard, Pieter D. de Koning, Inaki Morao
Publikováno v:
Synlett. 2010:873-876
This paper describes the large-scale synthesis of a progesterone receptor metabolite. The key step in this sequence was the regioselective pyrazole N-alkylation.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ebd9209195d15fad58263d91b8c874b8
https://doi.org/10.1055/s-0029-1219535
https://doi.org/10.1055/s-0029-1219535
Autor:
Yann C. Lecouturier, Patrick S. Johnson, David J. McManus, Toby J. Underwood, Pieter D. de Koning, Aurelie A. Robin, Paul A. Bradley
Publikováno v:
Organic Process Research & Development. 13:848-853
The development and implementation of a scaleable process for the manufacture of the nonsteroidal progesterone receptor antagonist 8 is described. Key aspects of the synthesis include (i) a telescoped chlorination−etherification sequence to prepare
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f8253c85beb53be0a659af1112204f3d
https://doi.org/10.1021/op900110k
https://doi.org/10.1021/op900110k