Faler Catherine A, Joullié Madeleine M
Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104-6323, USA.
Org Lett. 2007 May 10;9(10):1987-90. doi: 10.1021/ol0705907. Epub 2007 Apr 21.
An intermolecular Ti(IV)-mediated cyclopropanation reaction has been used to synthesize substituted 2-phenylcyclopropylamines and constrained analogues of the neurotransmitters histamine and tryptamine. Many hydroxy- and methoxy-substituted phenylcyclopropylamines are known to inhibit monoamine oxidase and have been shown to mimic hallucinogens. These compounds were made in 1 to 5 steps from readily available starting materials.
分子间钛（IV）介导的环丙烷化反应已被用于合成取代的2-苯基环丙胺以及神经递质组胺和色胺的受限类似物。许多羟基和甲氧基取代的苯基环丙胺已知可抑制单胺氧化酶，并已显示出具有致幻剂的模拟作用。这些化合物由易得的起始原料经1至5步反应制得。
