Polycyclic N-heterocyclic compounds. Part 75: Synthesis of 2,4-disubstituted 5,6-dihydro[1]benzoxepino[5,4-d]pyrimidines and 12-substituted 1,2,4,5-tetrahydro[1]benzoxepino[4,5-e]imidazo[1,2-c]pyrimidines as potential antiplatelet aggregators

Kensuke Okuda, Yuko Yamamoto, Takashi Hirota, Kenji Sasaki

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Abstract

Libraries of tricyclic 2-substituted 4-alkylamino-5,6-dihydro[1] benzoxepino[5,4-d]pyrimidines and tetracyclic 12-substituted 1,2,4,5-tetrahydro[1]benzoxepino[4,5-e]imidazo[1,2-c]pyrimidines were synthesized as part of our research to develop new effective antiplatelet drugs. Several alkyl and aryl groups were used as substituents at the 2-position. Evaluation of the effects of the newly synthesized compounds on collagen-induced platelet aggregation revealed several promising antiplatelet candidates with potencies superior to aspirin.

Original languageEnglish
Pages (from-to)972-981
Number of pages10
JournalJournal of Heterocyclic Chemistry
Volume51
Issue number4
DOIs
Publication statusPublished - 2014

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Heterocyclic Compounds
Pyrimidines
Platelet Aggregation Inhibitors
Platelets
Aspirin
Collagen
Agglomeration
imidazo(1,2-c)pyrimidine

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

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title = "Polycyclic N-heterocyclic compounds. Part 75: Synthesis of 2,4-disubstituted 5,6-dihydro[1]benzoxepino[5,4-d]pyrimidines and 12-substituted 1,2,4,5-tetrahydro[1]benzoxepino[4,5-e]imidazo[1,2-c]pyrimidines as potential antiplatelet aggregators",
abstract = "Libraries of tricyclic 2-substituted 4-alkylamino-5,6-dihydro[1] benzoxepino[5,4-d]pyrimidines and tetracyclic 12-substituted 1,2,4,5-tetrahydro[1]benzoxepino[4,5-e]imidazo[1,2-c]pyrimidines were synthesized as part of our research to develop new effective antiplatelet drugs. Several alkyl and aryl groups were used as substituents at the 2-position. Evaluation of the effects of the newly synthesized compounds on collagen-induced platelet aggregation revealed several promising antiplatelet candidates with potencies superior to aspirin.",
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T1 - Polycyclic N-heterocyclic compounds. Part 75

T2 - Synthesis of 2,4-disubstituted 5,6-dihydro[1]benzoxepino[5,4-d]pyrimidines and 12-substituted 1,2,4,5-tetrahydro[1]benzoxepino[4,5-e]imidazo[1,2-c]pyrimidines as potential antiplatelet aggregators

AU - Okuda, Kensuke

AU - Yamamoto, Yuko

AU - Hirota, Takashi

AU - Sasaki, Kenji

PY - 2014

Y1 - 2014

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