2-Deoxyribose as a Rich Source of Chiral 5-Carbon Building Blocks
摘要:
[GRAPHICS]We have developed concise routes to a number of useful chiral 5-carbon synthetic building blocks using readily available: 0-1-methyl-2-deoxyribose as starting material. Novel transformations include the use of indium triflate to catalyze the oxidation of a methyl furanoside to the corresponding lactone with MCPBA and the Vasella-type fragmentation of a 5-iodo furanoside using chromium(II) chloride when zinc proved ineffective. In addition, 3,4-disubstitued piperidine derivatives were prepared without hydroxyl group protection via a simple reductive amination reaction.
2-Deoxyribose as a Rich Source of Chiral 5-Carbon Building Blocks
摘要:
[GRAPHICS]We have developed concise routes to a number of useful chiral 5-carbon synthetic building blocks using readily available: 0-1-methyl-2-deoxyribose as starting material. Novel transformations include the use of indium triflate to catalyze the oxidation of a methyl furanoside to the corresponding lactone with MCPBA and the Vasella-type fragmentation of a 5-iodo furanoside using chromium(II) chloride when zinc proved ineffective. In addition, 3,4-disubstitued piperidine derivatives were prepared without hydroxyl group protection via a simple reductive amination reaction.
[EN] PYRAZOLE DERIVATIVES AS SGC STIMULATORS<br/>[FR] DÉRIVÉS DE PYRAZOLE UTILISÉS COMME STIMULATEURS DE SGC
申请人:IRONWOOD PHARMACEUTICALS INC
公开号:WO2016044447A1
公开(公告)日:2016-03-24
There are described imidazole and pyrazole derivatives which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
The invention provides a compound of formula I:
wherein A
1
, A
2
, A
3
, R
1
, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
The invention provides a compound of formula I:
wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
Azaquinazoline Inhibitors of Atypical Protein Kinase C
申请人:Cancer Research Technology Limited
公开号:US20140113882A1
公开(公告)日:2014-04-24
The present application provides a compound of formula (I)
or a salt thereof, wherein R
7
, R
8
, R
9
, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.