Tetrahedron

Large scale synthesis and absolute configuration of (-)-3-ppp, a selective dopamine autoreceptor agonist

SO Thorberg, L Gawell, I Csöregh, JLG Nilsson

Index: Thorberg; Gawell; Csoregh; Nilsson Tetrahedron, 1985 , vol. 41, # 1 p. 129 - 139

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Citation Number: 19

Abstract

A large scale synthesis for (-)-3-PPP has been developed. The racemic methoxy compound 1 was prepared in a three step procedure in 63% yield. This was resolved as a diastereomeric salt by crystallization of the (-)-di-p-toluoyltartrate. Two crystallizations gave the pure (-)-enantiomer 2 in 50% of the theoretical yield and with an enantiomeric excess of> 95%. Demethylation using aqueous HBr gave (-)-3-PPP,(3). Compound 2 was also ...