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.
AMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS
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, (2016/09/22)
The present invention relates to compounds of formula (I), including their stereoisomers and pharmaceutically acceptable salts. This invention also relates to methods of making such compounds and pharmaceutical compositions comprising such compounds. The compounds of this invention are useful in the treatment of various disorders that are related to 5-hydroxytryptamine 4 (5-HT4) receptor.
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.
(S)-4-amino-5-chloro-3-iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)b enzamide (TRIZAC), a high-affinity ligand for the 5-HT-3 receptor
De Paulis, Tomas,Trivedi, Bakula L.,Zhang, Zhang-Jin,Schmidt, Dennis E.,Ebert, Michael H.,Hewlett, William A.
, p. 2657 - 2662 (2007/10/03)
TRIZAC is one of the most potent 5-HT-3 receptor antagonist reported to date, having 20-fold higher affinity than (S)-5-iodozacopride. This high affinity (K(i) 0.05 ± 0.01 nM) and a moderate apparent lipophilicity (log P(app) 2.12) makes TRIZAC a promising ligand for studying 5-HT-3 receptors.
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;