Synthesis and purification of valacyclovir

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 473/18 (2006.01)

Patent

CA 2649826

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.

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