143878-24-4Relevant articles and documents
Preparation method of key intermediate 4-amino-5-halobenzofuran-7-carboxylic acid of 5-HT4 receptor stimulant
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, (2020/03/02)
The invention discloses a preparation method of a key intermediate 4-amino-5-halobenzofuran-7-carboxylic acid of a 1,5-HT4 receptor stimulant, belonging to the field of organic synthesis. According tothe preparation method, para-protected amino-o-hydroxybenzoic acid/hydroxybenzoate, a halogenating reagent and triethyl acetenyl silicon are used as main raw materials, and a three-step reaction is performed to obtain the 4-amino-5-halobenzofuran-7-carboxylic acid. The method has the advantages of simple process operation, short reaction steps, easy separation of the intermediate, total yield ofmore than 51%, usage cheap and easily available raw materials and greatly reduced production cost; and thus, the method has obvious competitive advantages.
NOVEL COMPOUND
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Page/Page column 12; 29, (2008/06/13)
The present invention relates to a novel benzofuran carboxamide derivative having pharmacological activity, to processes for its preparation, to compositions containing it and to its use in the treatment of diseases treatable by 5-HT4 agonism.
Process for the preparation of substituted benzofuran derivatives
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, (2008/06/13)
Substituted benzofuran derivatives of the formula (I): STR1 wherein one of R1 and R2 is hydrogen or halogen and the other is, independently, an amino group or a C2 -C4 alkanoyl amino group; R3 is hydrogen; a linear or branched C1 -C4 alkyl, C1 -C4 alkoxy or C2 -C4 alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C1 -C4 alkyl group; A is a group --(CH2)n -Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms, and n is zero or an integer of 1 to 3; and the symbol ..... represents a single or double bond; may be prepared by a process comprising reacting a compound of formula II: STR2 in which L is a leaving group and R4 is hydrogen or a carboxy protecting group, with a compound of formula III; to obtain a compound of formula IV; STR3 which is then cyclized to obtain a compound of formula V; STR4 which is reacted with a compound of formula VI;