PROCESS FOR THE PREPARATION OF 9-DEAZAGUANINE DERIVATIVES
摘要
Derivatives of 9-deazaguanine are prepared by reacting an aldehyde or ketone with a dialkylaminomalonate to form the corresponding enamine. The enamine is then reacted with a base to form a cyclic pyrrole. The cyclic pyrrole is reacted with an urea compound or a derivative of carbamimidoic acid to provide a protected guanidino compound. The guanidino is converted to the desired 9-deazaguanine derivative by reacting with trifluoracetic acid or with an alkoxide or hydroxide followed by neutralization with an acid.
申请公布号
WO9721653(A1)
申请公布日期
1997.06.19
申请号
WO1996US19556
申请日期
1996.12.12
申请人
BIOCRYST PHARMACEUTICALS, INC.;ELLIOTT, ARTHUR, J.;WALSH, DAVID, A.;MORRIS, PHILIP, E.
发明人
ELLIOTT, ARTHUR, J.;WALSH, DAVID, A.;MORRIS, PHILIP, E.