Development and Kilogram-Scale Synthesis of a D2/5-HT2A Receptor Dual Antagonist (±)-SIPI 6360
摘要:
The kilogram-scale synthesis of a D-2/5-HT2A receptor dual antagonist (+/-)-SIPI 6360 was developed as an alternative treatment for schizophrenia. Specifically, three conditions were modified and optimized, including the Vilsmeier conditions, to prepare quinoline 3. In addition, the palladium-catalyzed hydrogenation was modified to synthesize dihydroquinolin-2(1H)-one 5, and the reduction of beta-chloroamide was altered to form 3-chloropropanamine 8. Ultimately these improvements led to the preparation of a 1.5 kg of (+/-)-SIPI 6360 batch in eight steps with an overall yield of 34% and purity of 99.8%.
Protective Agent for Retinal Neuronal Cell Comprising Indazole Derivative as Active Ingredient
申请人:Seike Hisayuki
公开号:US20090012123A1
公开(公告)日:2009-01-08
As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.
Copper-catalyzed Goldberg-type C–N coupling in deep eutectic solvents (DESs) and water under aerobic conditions
作者:Luciana Cicco、Jose A. Hernández-Fernández、Antonio Salomone、Paola Vitale、Marina Ramos-Martín、Javier González-Sabín、Alejandro Presa Soto、Filippo M. Perna、Vito Capriati、Joaquín García-Álvarez
DOI:10.1039/d0ob02501a
日期:——
A scalable CuI-catalyzed Goldberg C–N coupling between aryl iodides and amides is reported either in DESs or in water.
报道了一种可扩展的CuI催化的高伯格C-N偶联反应,可在深共熔剂或水中进行。
[EN] THERAPEUTIC COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS THÉRAPEUTIQUES ET LEURS UTILISATIONS
申请人:GENENTECH INC
公开号:WO2016055028A1
公开(公告)日:2016-04-14
The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
The convenient aqueous synthesis and biological evaluation of ortho-(3,4,5-trimethoxybenzoyl)-acetanilides as novel anti-cancer agents
作者:Jianfei Sheng、Fei Mao、Jun Yan、Ling Huang、Xingshu Li
DOI:10.1039/c4ra07998a
日期:——
A series of newortho-(3,4,5-trimethoxybenzoyl)-acetanilides were synthesised by the cross-coupling reaction catalyzed with Pd catalyst in aqueous medium, with polyethylene glycol as additive under very mild conditions.
[EN] PRO-SURVIVAL COMPOUNDS<br/>[FR] COMPOSÉS FAVORISANT LA SURVIE
申请人:UNIV GLASGOW
公开号:WO2016092327A1
公开(公告)日:2016-06-16
Disclosed herein are a class of compounds useful in cell culture, in particular, the in vitro culture of stem cells. The compounds have been found to promote the survival and/or maintenance of stem cells in (or during) culture and/or throughout passage.