METHOD OF SYNTHESIS OF DERIVATIVES OF N-(3-HYDROXY-4-PIPERIDINYL)-(DIHYDROBENZOFURAN, DIHYDRO-2H-BENZOPYRAN OR DIHYDROBENZODIOXINE)-CARBOXAMIDE, OR THEIR SALTS, OR THEIR STEREOCHEMICALLY ISOMERIC FORM Russian patent published in 1995 - IPC

Abstract RU 2037492 C1

FIELD: organic chemistry. SUBSTANCE: product: derivatives of N-(3-hydroxy-4-piperidinyl)-(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxine)-carboxamide of the formula (I) where R1, R2, R3, L and A have corresponding meanings. Reagent 1: compound of the formula (II) where R1, R2, R3, L and A have corresponding meanings. Reagent 2: L-W, L has corresponding meanings, W halogen atom or sulfonylhydroxy-group; or aldehyde L′=0 where L′=0 are compound of the formula L-H in which two adjacent hydrogen atoms in C1-C6-alkanediyl or C3-C6-cycloalkanediyl were substituted with O, or alkene of the formula NC-CH=CH2. Process is carried out in the medium of inert solvent, nonobligatory in the presence of base, iodide salt or reducing agent following by conversion of one end product to the other, isolation of the end product in the free form or in the form of therapeutically active nontoxic salt, or in the form stereochemically isomeric form. Synthesized compounds were used in medicine, in gastroenterology. EFFECT: improved method of synthesis. 5 tbl

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RU 2 037 492 C1

Authors

Zhorzh Anri Pol' Van Del'[Be]

Frans Marija Al'Fons Van Den Kejbus[Be]

Dates

1995-06-19Published

1990-03-21Filed