Interaction of Aryloxychlorocarbenes with Acetylenedicarboxylate: Novel Formation of Polyfunctional Butadienes and 8-Oxatricyclo[3.2.1.02.4]oct-6-enes
摘要:
The interaction of aryloxychlorocarbenes with dialkyl acetylenedicarboxylates has been examined. Thermolyses of 3-aryloxy-3-chlorodiazirines in the presence of acetylenedicarboxylate resulted in the formation of unexpected polyfunctional 1,3-butadienes and 8-oxatricyclo[3.2.1.0(2.4)]oct-6-enes or of 2-aryoxycarbonylmaleates dependent upon reaction conditions. This work confirmed the nucleophilicity of aryloxychlorocarbenes and underlined their synthetic potential.
solvent‐free approach for the synthesis of 2‐aryloxypyridines with good to excellent yields has been developed by the reaction of 1,6‐diynes with aryl cyanates. This atom‐economical catalytic strategy offers a mild and practical approach to access a variety of such cycloadducts with excellent regioselectivities. The protocol was further extended to the synthesis of 2,2′‐ and 2,3′‐diaryloxybipyridines by the
Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure:
where the definitions of the variables are provided herein.
Formula I的Chroman化合物和衍生物是TRPM8的有用抑制剂。这些化合物在治疗多种由TRPM8介导的疾病和症状方面具有用途,并可用于制备治疗这些疾病和症状的药物和药物组合物。这些疾病的例子包括,但不限于,偏头痛和神经病性疼痛。Formula I的化合物具有以下结构:变量的定义在此提供。
BENZOPIPERAZINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS
申请人:Forma Therapeutics, Inc.
公开号:US20150232465A1
公开(公告)日:2015-08-20
The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I):
wherein X, Y, Z, R
1
, R
2
, R
4
and R
7
are defined herein.
Under neat conditions, an efficient method for synthesis of imidoesters has been developed using cyanatobenzenes and dicarbonyl compounds. Nucleophilic addition spontaneously occurred between the two kinds of materials at room temperature with yields of up to 90%. A mechanism directed towards to the imidoester formation has been proposed. (C) 2014 Yan Xiong. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.