Synthesis And Purification Of Valacyclovir

Abstract: The present invention relates to protected valacyclovir, N-tert-butoxycarbonyl-L-valine 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy] ethyl ester, and a method of making it. The present invention further relates to a method of making valacyclovir including the steps of coupling an amine protected valine selected from N-tbutoxycarbonyl valine and N-formyl valine with acyclovir using a coupling agent to form a protected valacyclovir, and deprotecting the protected valacyclovir to form valacyclovir or a pharmaceutically acceptable salt thereof. The present invention further relates to valacyclovir in pure form, a method of making pure valacyclovir, and to compositions containing pure valacyclovir.

Patent Information

Application #

Filing Date

11 May 2004

Publication Number

11/2007

Publication Type

INA

Invention Field

PHARMACEUTICALS

Status

Email

Parent Application

Applicants

TEVA PHARMACEUTICAL INDUSTRIES LTD.

5 BASEL STREET, P.O. BOX 3190, 49131 PETAH TIQVA ISRAEL

Inventors

1. MARINA, YU ETINGER,

HA-SAVION 14/1, NESHER 36822 ISRAEL

2. LEV, M. YUDOVICH,

TAANACH 24/10, HAIFA 32161 ISRAEL

3. MICHAEL YUZEFOVICH

YAD LABANIM 198/9, HAIFA 32687 ISRAEL

4. GENNADY, A. NISNEVICH

NETIV HEN 81/70, HAIFA 32688 ISRAEL

5. BEN, ZION DOLITZKI

LOCHAME-HAGETO ST., PETACH-TIQVA 49651 ISRAEL

6. BORIS PERTSIKOV,

NETIV HARIMON NESHER 4, 36781 ISRAEL

7. BORIS TISHIN,

46/63 LEON BLUM STREET, HAIFA 33855 ISRAEL

8. DINA BLASBERGER,

HAVERED STREET 8/3, RAANANA 43523 ISRAEL