N-(lower alkyl)-2-(3'-ureidobenzyl)pyrrolidines and N-(lower alkyl)-2-(3'-ureidobenzyl)-5-(lower alkyl)pyrrolidines are useful for lowering intraocular pressure in mammals, for example, in the treatment of glaucoma.
N-(lower alkyl)-2-(3′-ureidobenzyl)pyrrolidines and N-(lower alkyl)-2-(3′-ureidobenzyl)-5-(lower alkyl)pyrrolidines of formula I
wherein
R¹ is lower alkyl and
R² is lower alkyl or hydrogen, or a pharmaceutically acceptable salt thereof, or any single isomer or mixture of isomers thereof, useful for lowering intraocular pressure in mammals, for example, in the treatment of glaucoma.
N-(低级烷基)-2-(3′-亚脲基苄基)吡咯烷和 N-(低级烷基)-2-(3′-亚脲基苄基)-5-(低级烷基)吡咯烷的式 I
其中
R¹ 是低级烷基
R²为低级烷基或氢,或其药学上可接受的盐,或其任何单一异构体或异构体混合物,可用于降低哺乳动物的眼内压,例如治疗青光眼。
Acetylenes as potential antarafacial components in concerted reactions. Formation of pyrroles from thermolyses of propargyl amines, of a dihydrofuran from a propargylic ether, and of an ethylidenepyrrolidine from a .beta.-amino acetylene
作者:Alfred Viola、John J. Collins、Nicholas Filipp、John S. Locke
DOI:10.1021/jo00071a015
日期:1993.9
A thermal cyclization of acetylenic compounds provides evidence for the ability of acetylenic links to act as antarafacial components in [2 + 2] processes. The cyclization competes with the normally favored acetylenic retro-ene reaction. Propargylic amines, without substituents whose presence would hinder a tight cyclic transition state, yield intermediate pyrrolines whose subsequent hydrogen elimination affords pyrroles in small amounts. The same process in 2-ethynyltetrahydropyran affords 8-oxabicyclo[3.2.1]octane in 35% yield. A related thermal reaction of N-methyl-3-hexyn-1-amine provides a quantitative transformation to N-methyl-2-ethylidenepyrrolidine in a nominal [2s + 2a + 2s + 2s] Mobius process, wherein the acetylenic unit is the antarafacial component. Evidence for concertedness in these reactions is discussed.
MUCHOWSKI, JOSEPH M.;CLARK, ROBIN D.;WATERBURY, L. DAVID
作者:MUCHOWSKI, JOSEPH M.、CLARK, ROBIN D.、WATERBURY, L. DAVID