Crystal modification of 2,4-diamino-6-hydroxymethylpteridine hydrobromide

US5760229A · kind A · utility

Assignee

• Heinrich Mack Nachf · DE

Inventors

• Carsten Wangnick · Waldkirch, DE
• Peter Merrath · Memmingen, DE

Key dates

• Filing date: Feb 7, 1996
• Grant date: Jun 2, 1998
• Expiry date: Feb 7, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D475/08
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A novel crystal modification of the compound 2,4-diamino-6-hydroxymethylpteridine hydrobromide and a process for its preparation and its use for preparing methotrexate. The novel crystal modification of 2,4-diamino-6-hydroxymethylpteridine hydrobromide is distinguished in particular by the fact that only one equivalent of the brominating agent triphenylphosphine dibromide is needed for brominating the 6-hydroxymethyl group. No reaction with the amino groups in the 2 and 4 positions takes place. This facilitates the reaction to give 2,4-diamino-6-pteridinyl derivatives such as methotrexate.