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Molecules 2012, 17(5), 5604-5614; doi:10.3390/molecules17055604
Article

Novel Synthesis of 8-Deaza-5,6,7,8-tetrahydroaminopterin Analogues via an Aziridine Intermediate

1, 1, 1, 1, 1, 1,2 and 1,*
Received: 10 April 2012 / Revised: 3 May 2012 / Accepted: 5 May 2012 / Published: 10 May 2012
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Abstract

An efficient method for the construction of the tetrahydrofolate skeleton is described. Starting from pterin analogues and aromatic amines, 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives and the heterocyclic benzoyl isosteres were synthesized via a novel aziridine intermediate. Following this method, the byproducts of carbon-nitrogen bond hydrogenolysis in traditional synthetic strategy can be completely avoided.
Keywords: tetrahydrofolate; aziridine; catalytic hydrogenation; solvent-free tetrahydrofolate; aziridine; catalytic hydrogenation; solvent-free
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Zhou, S.; Tian, C.; Li, C.; Guo, Y.; Wang, X.; Liu, J.; Zhang, Z. Novel Synthesis of 8-Deaza-5,6,7,8-tetrahydroaminopterin Analogues via an Aziridine Intermediate. Molecules 2012, 17, 5604-5614.

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