Synthesis of structurally diverse diarylketones through the diarylmethyl sp3 CH oxidation
摘要:
Under open-flask conditions, an efficient method to assemble a series of diversely functionalized diarylketones in the presence of commercially available NBS has been developed. Yields of up to 99% have been achieved employing diarylmethanes as starting material. Based on O-18-labeled experiment, the addition of stoichiometric water eventually leads to excellent yields in all carbonylation cases. (C) 2014 Elsevier Ltd. All rights reserved.
An efficient in situ prepared superacid BF3–H2O promoted benzylation of arenes using benzyl alcohols and acetates achieves various diarylalkanes.
一种高效的原位制备的超强酸BF3-H2O促进的芳烃苄基化反应,使用苄醇和醋酸酯制备各种二芳基烷烃。
NOVEL IMIDAZOLYLALKYLCARBONYL DERIVATIVES AS CALCIUM CHANNEL MODULATORS AND PREPARATION METHOD THEREOF
申请人:CHOI Kyung Il
公开号:US20090325979A1
公开(公告)日:2009-12-31
Disclosed are novel imidazolylalkylcarbonyl derivatives useful as calcium channel modulators and a preparation method of the same. Also disclosed is a method for the treatment of diseases by administering the above compounds based on their inhibitory activity against calcium channel.
NOVEL PYRAZOLYLMETHYLAMINE COMPOUNDS AS CALCIUM CHANNEL MODULATORS AND PREPARATION METHOD THEREOF
申请人:NAM Ghilsoo
公开号:US20100094006A1
公开(公告)日:2010-04-15
The present invention relates to pyrazolylmethylamine-piperazine derivatives and their pharmaceutically acceptable salts effective as calcium channel modulators and a method of manufacturing the same. The present invention also relates to the medicinal use of the above compounds as therapeutic treatment of diseases due to their effect as calcium channel modulators.
Synthesis of Diarylmethanes via Metal-Free Reductive Cross-Coupling of Diarylborinic Acids with Tosyl Hydrazones
作者:Xijing Li、Yuanyuan Feng、Lin Lin、Gang Zou
DOI:10.1021/jo302207b
日期:2012.12.7
that takes advantage of diarylborinic acids as a cost-effective alternative to arylboronicacids for synthesis of diarylmethanes through metal-free reductive cross-coupling with N-tosylhydrazones of aromatic aldehydes and ketones. The procedure tolerates hydroxyl, halide, amine, and allyl functionality, complementary to the transition-metal catalyzed cross-coupling techniques.
Benzhydrylpiperazine derivatives, processes for the preparation thereof and pharmaceutical compositions comprising the same
申请人:FUJISAWA PHARMACEUTICAL CO., LTD.
公开号:EP0113226A1
公开(公告)日:1984-07-11
The invention relates to benzhydrylpiperazine derivatives having the following general formula:
wherein
A is lower alkylene,
Z is benzhydryl optionally substituted with halogen, and
R' is amino, aryl, pyridyl, acyl or acylamino, in which the aryl group and pyridyl group are substituted with nitro, amino or acylamino, provided that Z is benzhydryl substituted with halogen, when R1 is amino, and to pharmaceutically acceptable salts thereof.
These compounds possess anti-allergic activities and are effective in the treatment of allergic symptoms.
The invention further relates to processes for the preparation of these compounds and to pharmaceutical compositions containing them.
本发明涉及具有以下通式的苯甲基哌嗪衍生物:其中 A 为低级亚烷基,Z 为可选被卤素取代的苯甲基,R'为氨基、芳基、吡啶基、酰基或酰氨基,其中芳基和吡啶基被硝基、氨基或酰氨基取代,但当 R1 为氨基时,Z 为被卤素取代的苯甲基,本发明还涉及其药学上可接受的盐类。 这些化合物具有抗过敏活性,可有效治疗过敏症状。 本发明还涉及制备这些化合物的工艺以及含有这些化合物的药物组合物。