Process for the Preparation of 1-([1,3]dioxolan-4-ylmethyl)-1H-pyrazol-3-ylamine

摘要

The present invention relates to a novel process for the preparation of of the formula (I) (I) wherein R1 and R2 are described herein. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds for treating diseases or conditions associated with inhibiting actin polymerization.;

主权项

1. A process for the preparation of a compound of the formula wherein R1 and R2 are independently selected from hydrogen, C1-6alkyl, C3-7cycloalkyl, C3-6alkenyl, or phenyl; wherein C1-6alkyl, cycloalkyl, C3-6alkenyl or phenyl is optionally be substituted by halogen, hydroxyl, C1-6alkoxycarbonyl, or phenyl; or R1 and R2, together with the carbon to which they are attached, form a C3-7cycloalkyl; comprising a) protecting 3-aminopyrazole to form a compound of formula (II); wherein R3 is C1-6alkyl, cycloalkyl or phenyl; b) substituting the protected 3-aminopyrazole of formula (II) at the 1 position to form a compound of formula (III); c) hydrolyzing the protected 3-aminopyrazole of formula (III) under basic conditions to form a compound of formula (I)