Method for Preparation of compounds antagonistic Peptide (CGRP calcitonin gene-related)

摘要

Claim 1: procedure for preparing compounds of General formula (2), in which R1 is a group of formula (3), in which R1.1 c1-3 represents h, alkyl, - C (o) - or benzyl, C (o) - O - or benzyl Tert Butyl, comprising the steps of: (a) Attach a compound of General formula (4), in which R1 is defined as indicated above, and x means a hydrogen Atom or a metal Atom selected from the Group consist Entity in Lithium, sodium, and potassium.A compound of General formula (5) in which R3 represents a radical imidazole or triazole, which is connected through a nitrogen Atom; (b) Isolating a compound of General formula (1) obtained in STEP (a), preferably by crystallization in a Solvent, and (c) even Present information in an appropriate Solvent Solid obtained in STEP (b).Claim 5: procedure for preparing compounds of General formula (1), wherein R1 represents a group of formula (3), in which R1.1 represents h, alkyl C1 - 3 or - C (o) - C (o) - benzyl, or Tert Butyl or benzyl, and R2 means a secondary Amine - nr2.1r2.2 May be selected S r2.1 and R2.2, independently of each other, the group consisting of c1-3 alkyl or benzyl, and can form the Group -nr2.1r2.2 in a cyclic Amine, which can be selected from the group consisting of (- 4 - 1 - 4 - metilpiperazin ILO, ILO, bencilpiperazin - 4 - 1 - 1 - ((ILO, c1-3 alkyl) - carbonyl) - piperazin - 4 - 1 - (ILO, T - butiloxicarbonil) - piperazin - 4 - ILO, 1 - (Benzyloxycarbonyl) - piperazin - 4 - 1 - Ilo Ilo, piperidin and Pir Rolidin - 1 - ILO, its Salts and solvates,That includes the steps of: (a) Attach a compound of General formula (4), in which R1 is defined as indicated above, and x represents a hydrogen Atom or a metal Atom selected from the group consisting of Lithium, sodium and potassium, or hydrate thereof with a Compound General formula (5) in which R3 represents a radical imidazole or triazoleIt is linked through a nitrogen Atom; (b) making a product originated in the step (a), of General formula (2), in which R1 is defined as mentioned before, a compound of General formula (6) in which R2 is defined as indicated above; and (c) pair To prepare compounds of General formula (1), in which R1.1 is a hydrogen Atom or a protecting Group is removed below present a compound of General formula (1), in which R1.1 represents one of the groups C (o) - O - C (o) - benzyl, or Tert Butyl benzyl or.