Synthesis of Diazipine and [3H]Diazipine

Synthesis of Diazipine and [3H]Diazipine

Diazipine and [3H]diazipine were synthesized as new 1, 4-dihydropyridine photoaffinity ligands containing a phenyldiazirine group. After simple high performance liquid chromatography separation, both compounds were purified in good overall yields. [3H]Diazipine (21.2Ci/mmol) was synthesized in two s...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 1991-07, Vol.39 (7), p.1860
Hauptverfasser: TAKI, Motohiko, KUNIYASU, Akihiko, NAKAYAMA, Hitoshi, KANAOKA, Yuichi
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container_start_page 1860
container_title Chemical & pharmaceutical bulletin
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creator TAKI, Motohiko
KUNIYASU, Akihiko
NAKAYAMA, Hitoshi
KANAOKA, Yuichi
description Diazipine and [3H]diazipine were synthesized as new 1, 4-dihydropyridine photoaffinity ligands containing a phenyldiazirine group. After simple high performance liquid chromatography separation, both compounds were purified in good overall yields. [3H]Diazipine (21.2Ci/mmol) was synthesized in two steps from commercially available [3H]ethanolamine. Diazipine competitively inhibited [3H]PN200-110 binding to the calcium channel of cardiac membranes with high affinity.
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title Synthesis of Diazipine and [3H]Diazipine
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