Berotralstat Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Berotralstat (BCX7353, discovered by BioCryst Pharmaceuticals using a structure-guided drug design strategy) is a synthetic plasma kallikrein inhibitor that is potent and highly selective over other structurally related serine proteases.

Synthese

Berotralstat (BCX-7353) can be prepared by Grignard reaction of magnesium [3-[bis(trimethylsilyl) amino]-4-fluorophenyl](bromido)magnesium with 3-formylbenzonitrile in THF to give secondary alcohol , which is condensed with Boc-protected acid in the presence of PyBrop and DIEA in DMF to yield the corre sponding amide. Chlorination of alcohol with SOCl2 in CH2Cl2, followed by condensation with cyclopropylmethan amine in acetonitrile at 70 °C affords secondary amine, which is N-deprotected with HCl in dioxane to yield racemic berotralstat. Resolution of racemate by preparative SFC gives (R)-berotralstat.

Berotralstat Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Berotralstat Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21586	55
BOC Sciences	16314854226; +16314854226	inquiry@bocsci.com	United States	19853	58
ShangHai Caerulum Pharma Discovery Co., Ltd.	18149758185 18149758185	sales-cpd@caerulumpharma.com	China	3504	58
Quality Control Solutions Ltd.	0755-66853366 13670046396	orders@qcsrm.com	China	18190	56
BioPharmaMatrix,Inc.	0510-86010668	sales@biopharmamatrix.com	China	4888	55
ShangHai Biochempartner Co.,Ltd	177-54423994 17754423994	2853530910@QQ.com	China	8000	62
Beijing xinyanhui pharmaceutical research and development co., LTD	13969155946	1461866103@qq.com	China	16111	58
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd	15317229551	15151849396@163.com	China	985	58
BEIJING INNO-TECH PHARMIC TECHNOLOGY CO.,LTD	15011485209		China	145	58
Chengdu PEIP Pharmaceutical Technology Co., LTD.	028-61715638 18011352545	1242335275@qq.com	China	459	58

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• Berotralstat
• Berotralstat (BCX-7353)
• 1H-Pyrazole-5-carboxamide, 1-[3-(aminomethyl)phenyl]-N-[5-[(R)-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl]-2-fluorophenyl]-3-(trifluoromethyl)-
• Berotralstat (BCX7353, BCX-7353)
• Berotralstat Crude
• (R)-1-(3-(Aminomethyl)phenyl)-N-(5-((3-cyanophenyl)((cyclopropylmethyl)amino)methyl)-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
• 1809010-50-1
• C30H26F4N6O