Probes for narcotic receptor mediated phenomena. 17. Synthesis and evaluation of a series of trans-3, 4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl) cyclohexyl] …

BR De Costa, RB Rothman, V Bykov…

Index: Costa, Brian R. de; Rothman, Richard B.; Bykov, Victor; Band, Linda; Pert, Agu; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 4 p. 1171 - 1176

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Citation Number: 18

Abstract

DCC coupling of (+)-and (-)-7 with nitrophenylacetic acids followed by catalytic hydrogenation and treatment with thiophosgene afforded a series of six isomeric aryl isothiocyanate analogues of U50, 488. Similarly, DCC coupling of (+)-and (-)-7 with (+)-and (- )-Nt-Boc-protected phenylglycines afforded four isomeric alkyl isothiocyanates. Evaluation of the isothiocyanates for their capacity to produce wash-resistant inhibition of M, 6, and K ...