- HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
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The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: Formula (I) which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions
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Page/Page column 159-160
(2017/08/07)
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- Synthetic method of 2-methyl-6-(4-methylphenyl)sulfonyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine
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The invention provides a synthetic method of 2-methyl-6-(4-methylphenyl)sulfonyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. According to the invention, compound 4-bromo-1-[(4-methylphenyl) sulfonyl]-1,2,3,4-tetrahydro-5H-1-benzazepine-5-one represented by formula I is reacted with acetamidine hydrochloride in the presence of cesium carbonate in a reaction solvent. The synthetic method comprises following advantages compared with the prior art, reaction temperature is lower, reaction time is shorter, and finished product yield and purity are both increased to certain degrees.
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Paragraph 0057; 0058; 0059
(2016/10/31)
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- A scalable process for the synthesis of 2-methyl-1,4,5,6- tetrahydroimidazo[4,5-d][1]benzazepine monohydrate and 4-[(biphenyl-2- ylcarbonyl)amino]benzoic acid: Two new key intermediates for the synthesis of the AVP antagonist conivaptan hydrochloride
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A process for the multikilogram synthesis of the dual vasopressin-receptor antagonist, conivaptan hydrochloride, has been developed. This method relies on the introduction of operationally simple chemistry during the final stages of the process when two k
- Tsunoda, Takashi,Yamazaki, Atsuki,Mase, Toshiyasu,Sakamoto, Shuichi
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p. 593 - 598
(2012/12/25)
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- A new synthetic route to YM087, an arginine vasopressin antagonist
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A new synthesis of N-{4-[(2-methyl-4,5-dihydroimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl} biphenyl-2-carboxamide monohydrochloride (1, YM087) via new imidazobenzazepine intermediates is described. This method remarkably improves the overall yiel
- Tsunoda, Takashi,Tanaka, Akihiro,Mase, Toshiyasu,Sakamoto, Shuichi
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p. 1113 - 1122
(2007/10/03)
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