Peter M. Munson

Design and synthesis of N-alkylated saccharins as selective α-1a adrenergic receptor antagonists☆

Abstract Benign prostatic hyperplasia can be managed pharmacologically with α-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the α-1 a receptor subtype may offer advantages in clinical applications with respect to hypotensive side effects. The N-alkylated saccharins reported here represent a new class of subtype selective α-1 a adrenergic receptor antagonists which demonstrate potent effects on prostate function in vivo and are devoid of blood pressure side effects.

A short synthesis of 3(r)-hydroxy-2(R)-isopropyltetrahydrothiophene: A precursor to a high-affinity P2-ligand of HIV-1 protease inhibitors

Abstract The title compound was synthesized in a 6 step sequence involving an efficient lipase-mediated resolution of racemic 3-hydroxy-2-isopropyltetrahydrothiophene.