129477-21-0Relevant articles and documents
A 5 - bromo -2 - methyl nicotinic acid ethyl ester
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Paragraph 0036-0047; 0056-0058, (2019/02/13)
The invention discloses a 5 - bromo - 2 - methyl nicotinic acid ethyl ester synthetic method, comprises the following steps: the acetyl ethyl acetate and alkali A adding solvent in the B enolizable; adding intermediate III and DABCO reaction; adding ammonium to cyclization; adding water quenching, organic solvent extraction C; removing the organic solvent to be crystalline crude product shall C; to be crystalline crude product recrystallized from 5 - bromo - 2 - methyl nicotinic acid ethyl ester; the invention to Meck development of 5 - chloro - 2 - methyl nicotinic acid ethyl ester is based on, through changing the reaction solvent and reduce the reaction temperature, significantly improves the stability of the intermediate III, so that the reaction can be smoothly to obtain the product, after treatment through recrystallization purification, thus avoiding the time-consuming column chromatography process, the average yield of 70%, the purity of 99.0% or more, is suitable for the large-scale industrial production.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND BENAMIDE COMPOUNDS AND DRUGS CONTAINING THE SAME
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Example 107, (2010/01/31)
Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases. In formula (I), R1 and R2 represent alkyl, alkoxy, cycloalkyl, phenyl, alkenyl, alkynyl, or a five- or six-membered saturated or unsaturated heterocyclic ring, or R1 and R2, together with a nitrogen atom to which R1 and R2 are attached, may form a ring; R3 and R4 represent a hydrogen atom, alkyl, a halogen atom, hydroxyl, nitrile, alkoxycarbonyl, alkoxy, or carboxyl; or R2 and R3 may be attached to each other to form -(CH2)m-, -N=CH-, -CH=N-, or -(C1-6 alkyl)C=N-; A, D, E, and G each represent a carbon atom, or any one of A, D, E, and G represents a nitrogen atom with the other three each representing a carbon atom; Q represents a nitrogen atom or a carbon atom; Y represents a group represented by formula (II) wherein X represents a hydrogen atom, group -C(=O)N(R5)R6 or group -C(=O)OR7, R8 is absent or represents a bond, an oxygen atom, a sulfur atom, -SO2-, -SO-, -CH2-CH2-, or - CH=CH-, and R9 and R10 represent a hydrogen atom, alkyl, alkoxy, a halogen atom, or hydroxyl; and Z represents - (CH2)n-, -O-(CH2)i-, or -C(=O)NH-(CH2)i-.