Zobrazeno 1 - 10
of 72
pro vyhledávání: '"Lianhe Shu"'
Publikováno v:
Organic Process Research & Development. 20:2050-2056
An efficient asymmetric synthesis of MDM2 antagonist RG7388 is reported. The highly functionalized chiral pyrrolidine carboxamide was assembled via a Cu(OAc)2/(R)-BINAP catalyzed asymmetric [3 + 2] cycloaddition, which gave the exo and endo adducts i
Publikováno v:
Organic Process Research & Development. 17:651-657
An efficient and practical synthesis of a naphthylacetic acid CRTH2 receptor antagonist is reported. Michael addition of ethyl t-butyl malonate to an allenoate afforded a triester, which was selectively hydrolyzed and decarboxylated to give a benzyli
Publikováno v:
Organic Process Research & Development. 17:247-256
A practical synthesis of a spiroindolinone pyrrolidinecarboxamide MDM2 antagonist 2 is reported. Cycloaddition of dipolarophile 3 with imine 30 afforded a complex mixture of diastereomers that were isomerized to the desired stereoisomer 31 by heating
Autor:
Lianhe Shu, Lady Mae Alabanza, James A. Wright, Yan Dong, Ping Wang, Roumen Nikolaev Radinov, Romyr Dominique
Publikováno v:
Organic Process Research & Development. 17:114-119
An improved, kilogram-scale synthesis of a LTB4 receptor antagonist is reported. The title compound was prepared in four linear steps (seven steps total) and 54% overall yield. The 3,5-bisarylphenol core was obtained in nearly quantitative yield by t
Publikováno v:
Organic Process Research & Development. 16:1940-1946
An improved, kilogram-scale synthesis of a triarylimidazoline MDM2 antagonist is reported. The nicotinic acid component was prepared in three steps from ethyl 2-dimethylaminomethylene-3-oxo-butyrate. The coupling of the nicotinic acid with the meso-d
Publikováno v:
Organic Process Research & Development. 16:1870-1873
A concise synthesis of a tetrahydropyrazolopyrazine building block is described. 5-Methyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-ylamine was prepared in three steps and 80% yield from 5-nitro-2H-pyrazole-3-carboxylic acid. This compound was then
Publikováno v:
Organic Process Research & Development. 16:1866-1869
A practical synthesis of cis-4,5-bis(4-chlorophenyl)imidazoline, a key intermediate for Nutlin analogues, is reported. The title compound was prepared in 81–88% yield by boric acid catalyzed direct condensation of meso-bis(4-chlorophenyl)ethane-1,2
Publikováno v:
The Journal of Organic Chemistry. 72:6320-6323
Asymmetric epoxidation of various olefins with an N-aryl-substituted oxazolidinone-containing ketone as catalyst and hydrogen peroxide as the primary oxidant has been investigated, and up to 96% ee was obtained.
Publikováno v:
Organic Letters. 5:293-296
[reaction: see text] Ketones containing N-aryl-substituted oxazolidinones have been prepared and investigated for the epoxidation of cis-beta-methylstyrene, styrene, and 1-phenylcyclohexene. The attractive interaction between the phenyl group of the
Publikováno v:
The Journal of Organic Chemistry. 67:2435-2446
This paper describes a new class of chiral oxazolidinone ketone catalyst for asymmetric epoxidation. High ee values have been obtained for a number of cyclic and acyclic cis-olefins. The epoxidation was stereospecific with no isomerization observed i