ES363453A1 - Procedure for producing a benzazocine derivative. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Procedure to produce a benzazocin derivative of formula: **(See formula)** (where R1 represents methoxy, hydroxy, or acyloxy, including the case where two groups together form an alcoholelenedioxy group; m is an integer from 1 to 3; R2 represents an alcohol group having at most 4 carbon atoms; and R4 represents a alcohol group having a maximum of 6 carbon atoms, an aralcohyl group having up to 10 carbon atoms, an alkoxylaminocarbonylalkyl or mono- or dialkoxylaminoalcohyl group in which the alcoholic group has a maximum of 3 carbon atoms, an acyl group having a maximum of 4 carbon atoms, a tetrahydrofurfuryl group or a hydrogen atom), which comprises reacting a phenylalkyl amine derivative of the formula: **(See formula)** (where R1, R4 and m have the same meanings defined above, and X'represents a radical (see formula) where R2 has the same meaning as before, or represents a functional group derived from a carboxylic group), with a Grignard reagent of formula R2MgX (where R2 has the same meaning defined above, and X represents a halogen), whereby the corresponding phenylalkyl amino alcohol derivative is produced, and subjecting the thus produced phenylalcoxylamino alcohol to a ring closure reaction, and optionally subjecting the thus produced benzazocine derivative to one or more of the following procedures: (1) reducing the group when the group is reducible; (2) when the group (s) (R1) m are alkoxy or acyloxy, convert them to hydroxyl groups; (3) when the group (s) (R1) m are hydroxyl group (s), convert them to alkoxy or acyloxy group (s). (Machine-translation by Google Translate, not legally binding)