A METHOD OF SYNTHESIZING CREATINE DERIVATIVES

摘要

A method of synthesizing (Boc)2-creatine derivatives of formula (III) which comprises a first step in which a sarcosine ester is reacted with a guanylating agent comprising two nitrogen atoms each protected with a t-butoxycarbonyl (t-Boc) group to form a (Boc)2-creatine ester, and a second step in which the (Boc)2-creatine ester is subjected basic hydrolysis to form (Boc)2-creatine of formula (III) is described. The (Boc)2-creatine so obtained can be used in methods of synthesizing creatine and phosphocreatine derivatives in which the free carboxyl group of the creatine is conjugated with a desired molecule.;

主权项

1. A method of synthesizing (Boc)2-creatine of formula (III), comprising the steps of:
(i) reacting a sarcosine ester of formula (I) wherein R is a linear or branched, saturated or unsaturated alkyl or aryl group having 1 to 8 carbon atoms, with a guanylating agent comprising two nitrogen atoms each protected with a t-butoxycarbonyl group (t-Boc), to form a (Boc)2-creatine ester of formula (II) wherein R is a linear or branched, saturated or unsaturated alkyl or aryl group having 1 to 8 carbon atoms; and (ii) subjecting the (Boc)2-creatine ester of formula (II) to basic hydrolysis, to form (Boc)2-creatine of formula (III)