- 4-(2-chloroethyl) thiazole-2-carboxylic acid ethyl ester and preparation method and application thereof
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The invention provides 4-(2-chloroethyl) thiazole-2-carboxylic acid ethyl ester and a preparation method and application thereof. The preparation method comprises the steps that 2-(2-aminothiazole-4-yl) ethyl acetate of a compound 1 is dissolved in dichloromethane, and 2-(2-bromothiazole-4-yl) ethyl acetate is obtained through diazotization and halogenation; then, under the condition of a reducing agent, 2-(2-bromothiazole-4-yl) ethane-1-ol is obtained; in a carbon monoxide atmosphere, carbonyl insertion reaction is performed through a proper catalyst to obtain 4-(2-ethoxyl) thiazole-2-carboxylic acid ethyl ester; and finally, thionyl chloride is used for chlorination to obtain 4-(2-chloroethyl) thiazole-2-carboxylic acid ethyl ester. The 4-(2-chloroethyl) thiazole-2-carboxylic acid ethyl ester can be used as an intermediate in synthesis of APJ receptor stimulant compounds. The invention provides a route method for synthesizing the 4-(2-chloroethyl) thiazole-2-carboxylic acid ethyl ester for the first time, the reaction condition is mild after the brominating reagent is optimized in the first step, and the yield is improved.
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- NLRP MODULATORS
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
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- NLRP MODULATORS
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein, useful to treat connected to the modulation of NRLP3.
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- HYDROXY CONTAINING FXR (NR1H4) MODULATING COMPOUNDS
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The present invention relates to compounds (1) which bind to the NR1 H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds (1) for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
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Page/Page column 92
(2016/07/05)
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- HETEROCYCLYL-SUBSTITUTED ANTI-HYPERCHOLESTEROLEMIC COMPOUNDS
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This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts thereof, wherein R12 is a hydroxylated alkyl group and R9 contains a heterocyclic ring. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating atherosclerosis and preventing atherosclerotic disease events.
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Page/Page column 41
(2008/12/05)
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