A Unified Continuous Flow Assembly-Line Synthesis of Highly Substituted Pyrazoles and Pyrazolines
作者:Joshua Britton、Timothy F. Jamison
DOI:10.1002/anie.201704529
日期:2017.7.17
molecular diversity in short order. Continuous flowsynthesis enables the safe handling of diazoalkanes at elevated temperatures, and the use of aryl alkyne dipolarphiles under catalyst-free conditions. This assembly-line synthesis provides a flexible approach for the synthesis of agrochemicals and pharmaceuticals, as demonstrated by a four-step, telescoped synthesis of measles therapeutic, AS-136A, in a total
Synthesis of 5 Trifluoromethyl‐1,4‐dihydro‐1,2,4‐triazines via Base‐mediated [3 + 3] Cycloaddition of Nitrile Imines and CF3−Imidoyl Sulfoxonium Ylides
An approach for the construction of 5-trifluoromethyl-1,4-dihydro-1,2,4-triazines has been developed via base-mediated [3+3] cycloaddition of in-situ generated nitrile imines and CF3-substituted imidoyl sulfoxonium ylides. The metal-free protocol is characterized by readily available starting materials, mild conditions, a broad substrate scope, high efficiency, good synthetic prospect, and scalability