Facile and Convenient Synthesis of N′¹,N′³-Dialkyl-N′¹,N′³-bis(arylcarbonothioyl)malonohydrazides via Propylphosphonic Anhydride Coupling

Dedicated to Professor Chengye Yuan and Professor Li-Xin Dai of the Shanghai Institute of Organic Chemistry (CAS) on the occasion of their 90^th birthdays

Abstract

A facile and convenient synthetic method for the anticancer agent elesclomol and its analogues, N′¹,N′³-dialkyl-N′¹,N′³-bis(arylcarbonothioyl)malonohydrazides, by the direct coupling of N-alkyl-N-(substituted)benzothiohydrazides and substituted malonic acids using propylphosphonic anhydride (T3P^®) under very mild conditions has been developed.

Key words

propylphosphonic anhydride - elesclomol - analogues - synthesis - anticancer agents

• References

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