(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.

A new method is described for synthesis of (Z)-7-eicosen-11-one (1) and (Z)-7-nonadecen-11-one (2), the active principles of the sex pheromone of the peach fruit moth, using the Wittig reaction for g-keto aldehydes prepared from diethyl…

A new method is described for synthesis of (Z)-7-eicosen-11-one (1) and (Z)-7-nonadecen-11-one (2), the active principles of the sex pheromone of the peach fruit moth, using the Wittig reaction for g-keto aldehydes prepared from diethyl…

A new method is described for synthesis of (Z)-7-eicosen-11-one (1) and (Z)-7-nonadecen-11-one (2), the active principles of the sex pheromone of the peach fruit moth, using the Wittig reaction for g-keto aldehydes prepared from diethyl…

A series of skeletal rearranged indolomorphinans 7a-d were obtained by N-demethylation of 3-methoxy-N-methyl-14-hydroxymorphinan-6-one 12 followed by N-realkylation, reduction and Fischer indole cyclization. The structure of the novel skeleton was…

3-(4-Chlorobenzyl)-8-methoxy-1,2,3,4-tetrahydrochromeno3,4-cpyridin-5-one (1), a putative dopamine D(4) receptor antagonist (k(i) = 8.7 nM), was labeled by positron-emitter (11C) and its pharmacological evaluation was carried out with in vitro…

We re-examined the accessory site of the 4,5-epoxymorphinan skeleton by camdas conformational analysis in an effort to deign novel delta opioid receptor antagonists. We synthesized three novel compounds (SN-11, 23 and 28) with a 10-methylene bridge…

Several neoclerodanes, such as salvinorin A (1) and herkinorin (3), have recently been shown to possess opioid receptor activity in vitro and in vivo. To explore the structure-affinity relationships of this interesting class of compounds, we have…

The dehydrophenylalanine4-enkephalin having the E-configuration (delta EPhe; phenyl and C = 0, cis) was prepared by photoisomerization of the Z-isomer with 3100 A light, followed by reversed-phase HPLC separation of the resulting mixture of the Z-…

Looking for hidden symmetry: The first asymmetric total synthesis of pentacyclic compounds 1 and 2 has been accomplished starting from a cyclic meso-anhydride. The absolute configuration of the final products was set by an organocatalytic…

Formula: see text 2-Methylaziridine-2-phosphonates were prepared from enantiopure sulfinimines and were demonstrated to be versatile synthetic intermediates for the synthesis of novel alpha-disubstituted and alpha,beta-trisubstituted…