125991-51-7Relevant articles and documents
Exploitation of a new route to fused pyrroles: Synthesis of TNP-351, homo-MTA and 5-arylpyrrolo[2,3-d]pyrimidines
Taylor, Edward C.,Liu, Bin
, p. 4027 - 4030 (2007/10/03)
We have developed a new methodology for the construction of pyrrolo[2,3- d]pyrimidines that involves Michael addition of 2,6-diamino-4(3H)- pyrimidinone or 2,4,6-triaminopyrimidines to nitroolefins, followed by a Nef reaction of the resulting adduct to form an intermediate aldehyde that spontaneously cyclizes to the fused pyrrole ring. This methodology has been exploited in a new synthesis of TNP-351, and for the first reported preparation of homo-MTA and of a series of 5-arylpyrrolo[2,3-d]pyrimidines.
A Novel Synthetic Approach to Pyrrolopyrimidine Antifolates
Miwa, Tetsuo,Hitaka, Takenori,Akimoto, Hiroshi
, p. 1696 - 1701 (2007/10/02)
A novel and efficient synthetic method for the synthesis of pyrrolopyrimidine antifolates is described.The key reaction of this method is the photo-initiated free radical addition of bromomalononitrile or ethyl bromocyanoacetate to an enol ether to afford the backbone skeleton of the targeted antifolate molecule.The key intermediates 3 or 4 are smoothly converted to the pyrrolopyrimidine antifolates 1 or 2 in three steps and in high overall yield.
Novel Pyrrolopyrimidine Antifolates: Synthesis and Antitumor Activities
Miwa, Tetsuo,Hitaka, Takenori,Akimoto, Hiroshi,Nomura, Hiroaki
, p. 555 - 560 (2007/10/02)
New antifolates, characterized by a 6-5 fused ring system, a pyrrolopyrimidine ring, and a trimethylene bridge at position 5 (12a,b and 13a,b) were designed and efficiently synthesized.The synthetic method included (1) construction of the key inter
