- Synthesis and in-vitro anti-proliferative evaluation of some pyrazolo[1,5-a]pyrimidines as novel larotrectinib analogs
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A series of 2-phenyl-7-(aryl)pyrazolo[1,5-a]pyrimidine-3-carbonitriles 11a–j and 2-phenyl-7-(aryl)pyrazolo[1,5-a]pyrimidine-3,6-dicarbonitriles 16a–c was synthesized by the reaction of 5-amino-3-phenyl-1H-pyrazole-4-carbonitrile (5) with 3-(dimethylamino)
- Attia, Mohamed H.,Elrazaz, Eman Z.,El-Emam, Soad Z.,Taher, Azza T.,Abdel-Aziz, Hatem A.,Abouzid, Khaled A.M.
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- Studies with functionally substituted enamines: Synthesis of 2-aroyl-3-dimethylamino-2-propenenitrile and their reactivity toward nitrogen nucleophiles
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A facile and efficient synthesis of 2-substituted 3-dimethylamino-2-propenenitrile 4a-c is described. Reaction of 4a-c with hydrazine hydrate afforded 3-substituted-1H-4-pyrazole carbonitrile 9a-c. Compounds 4a-c reacted with 5-methyl-1H-pyrazol-3-amine to give 7-substituted pyrazolo[1,5-a]pyrimidine-6-carbonitrile 12a-c and 2-substituted 5-aminopyrazolo[1,5-a]pyrimidine 16a,b, and with 1H-benzo[d]imidazol-2-amine to give 3-substituted 2-aminobenzo[4,5]imidazo[1,2-a]pyrimidine 19a,b and 4-substituted benzo[4,5]imidazo[1,2-a]pyrimidine 3-carbonitrile 21c. The structures of compounds obtained were deduced based on 1HNMR, HMBC-15N and NOE difference experiments.
- Al-Qalaf, Fawzia,Abdelkhalik, Mervat Mohammed,Al-Enezi, Amal,Al-Ajmi, Johara Rashed
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p. 145 - 156
(2008/09/20)
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- Method of using substituted pyrazolo [1,5-a] pyrimidines
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This invention relates to novel methods of use of certain pyrazolo[1,5-a]pyrimidine compounds and the therapeutically acceptable salts thereof. This invention also relates to novel methods of using these compounds as anti-proliferative agents in mammals, including humans.
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Page/Page column 45
(2010/10/20)
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