Preparation method of silodosin key intermediate

Preparation method of silodosin key intermediate

The invention discloses a preparation method of a silodosin key intermediate, and belongs to the technical field of medicine synthesis. Carrying out Friedel-Crafts reaction on indoline and trichloroacetonitrile to obtain a compound 1; brominating to obtain a compound 2; then carrying out substitutio...

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Hauptverfasser: YUAN RUNBO, QI XIAOMING, LI YUANYUAN, LUO YONGFENG
Format: Patent
Sprache:chi ; eng
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ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator YUAN RUNBO
QI XIAOMING
LI YUANYUAN
LUO YONGFENG
description The invention discloses a preparation method of a silodosin key intermediate, and belongs to the technical field of medicine synthesis. Carrying out Friedel-Crafts reaction on indoline and trichloroacetonitrile to obtain a compound 1; brominating to obtain a compound 2; then carrying out substitution with 2-(3-bromopropoxy) tetrahydro-2H-pyran to obtain a compound 3; then carrying out nucleophilic addition with (S)-epoxypropane or (R)-epoxypropane at an ultralow temperature to obtain a compound 4; then carrying out Mitsunobu reaction with phthalimide to obtain a compound 5 (configuration inversion) or esterifying with paratoluensulfonyl chloride, and reacting with potassium phthalimide under the condition of inorganic alkali to obtain the compound 5; reducing through hydrazine hydrate to obtain a compound 6; then removing tetrahydropyran protection from p-toluenesulfonic acid to obtain a compound 7; performing amino Boc protection under an alkaline condition to obtain a compound 8; esterifying with benzoyl ch
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title Preparation method of silodosin key intermediate
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