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Overview

The for diastereomers of N-(1,3,4,6,7,11b-hexahydro-7-phenyl-2H-benzo[a]quinolizin-2-yl)-N-phenylpropanamide (7c, 7d, 9c, and 9d), which are conformationally restricted analogues of fentanyl, were synthesized and separately tested for analgesic activity and affinity for the opiate receptor of rat brain. Stereochemical assignments for 7c, 7d, 9c, and 9d were deduced from NMR spectral analyses. Conformational analysis revealed that the 2 alpha isomers (7d and 9d) exist in solution as mixtures of cis- and trans-fused conformers with ca. 90 and 45% cis form, respectively. Other compounds (12a, 12b, and 14) related to these propionanilides were also prepared, stereochemically characterized, and tested. Weak analgesic activity was observed for 7d, and both 7d and 9d bound to the opiate receptor with an I50 of ca. 1100 and 1500 nM, respectively (ca. 0.5% of fentanyl and 2% of morphine). The analgesic activity of 7d was abolished by the opiate antagonist naloxone.

01 Jan 1981·Analytical Profiles of Drug Substances

Haloperidol

Author: Janicki, Casimir A. ; Ko, Chan Yan

A review with 69 references on the description, phys. properties, synthesis, stability, metabolism, and anal. of haloperidol (I) [52-86-8].

01 Jan 1981·The Journal of Organic Chemistry

Properties of bis(trifluoroacetoxy)borane as a reducing agent of organic compounds

Author: Maryanoff, Bruce E. ; Nortey, Samuel O. ; McComsey, David F.

(CF₃CO₂)₂BH-THF reduced indoles, ketones, aldehydes, imines, and compounds that readily generate carbocations in CF₃CO₂H.On the other hand, epoxides and ortho esters decomposed under the reaction conditions.Olefins and acetylenes were not hydroborated, and carboxylic acids were not reduced.

100 Deals associated with McNeil Laboratories

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100 Translational Medicine associated with McNeil Laboratories

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Pipeline

Pipeline Snapshot as of 22 Aug 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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