1449300-08-6Relevant articles and documents
Intermolecular Reductive Heck Reaction of Unactivated Aliphatic Alkenes with Organohalides
Zheng, Kewang,Xiao, Guanlin,Guo, Tao,Ding, Yalan,Wang, Chengdong,Loh, Teck-Peng,Wu, Xiaojin
, p. 694 - 699 (2020)
A general intermolecular reductive Heck reaction of organohalides with both terminal and internal unactivated aliphatic alkenes has been first realized in high yield with complete anti-Markovnikov selectivity. The challenging vinyl bromides, aryl chlorides, and polysubstituted internal alkenes were first applied. More than 100 remote carbofunctionalized alkyl carboxylic acid derivatives were rapidly synthesized from easily accessible starting materials. The synthesis of drug molecules has further demonstrated the wide synthetic utility of this scalable strategy. Preliminary mechanistic studies are consistent with the proposed catalytic cycle.
Tungsten-Catalyzed Transamidation of Tertiary Alkyl Amides
Feng, Fang-Fang,Liu, Xuan-Yu,Cheung, Chi Wai,Ma, Jun-An
, p. 7070 - 7079 (2021/06/30)
Transamidation has recently emerged as a straightforward and convenient means to diversify amides. However, the kinetically and thermodynamically demanding transamidation of notoriously robust, fully alkyl-substituted tertiary amides still remains a longstanding challenge. Here, we describe a method for the activation of tertiary alkyl amides to streamline transamidation using simple tungsten(VI) chloride as a catalyst and chlorotrimethylsilane as an additive. The highly electrophilic and oxophilic tungsten catalyst enables the selective scission of a C-N bond of tertiary alkyl amides to effect transamidation of a myriad of structurally and electronically diverse tertiary alkyl amides and amines. Mechanistic study implies that the synergistic effect of the catalyst and the additive could pronouncedly induce the nucleophilic acyl substitution of tertiary alkyl amide with amine to realize transamidation.
Method for simply, conveniently and efficiently synthesizing 4-arylbutyric acid derivative
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Paragraph 0027-0029; 0058, (2021/01/15)
Disclosed is a method for simply, conveniently and efficiently synthesizing 4-arylbutyric acid derivative. According to the method, removable 8-aminoquinoline is used as a guide group to control the regioselectivity of the reaction, and non-activated 3-butene amide is used as a reaction raw material to react with cheap, easily available, stable and efficient aryltrimethoxysilane, and a series of functionalized 4-aryl butyric acid derivatives can be simply and efficiently prepared and synthesized. The method is simple and convenient to operate, reaction raw materials are simple and easy to obtain, the product is easy to separate and purify, the product yield is high, and reaction regioselectivity is good. The invention can provide related products for treating urea circulation disorder, novel anti-type II diabetes mellitus drugs, angiotensin converting enzyme inhibitors and the like, and has good market potential and application value.
