藥物詳細合成路線

Name	Talipexole dihydrochloride;BHT-920;B-HT-920;Domin
Chemical Name	6-Allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine dihydrochloride
CAS	36085-73-1
Related CAS	101626-70-4 (free base)
Formula	C10H17Cl2N3S
Structure
Formula Weight	282.23709
Stage	上市-1996
Company	Boehringer Ingelheim (Originator)
Activity/Mechanism	Antiparkinsonian Drugs, Extrapyramidal Disorders, Treatment of, NEUROLOGIC DRUGS, alpha2-Adrenoceptor Agonists, Dopamine Autoreceptor Agonists, Dopamine D2 Agonists
Syn. Route	1

Route 1 the bromination of 1-allylhexahydro-4h-azepin-4-one (i) with br2 in acetic acid gives 1-allyl-5-bromohexahydro-4h-azepin-4-one (ii), which is cyclized with thiourea (iii) in refluxing ethanol. List of intermediates No. methyl (1s,3as,4s,5s,7as)-4-(cyanomethyl)-7a-methyl-5-[(1r,3r,6r)-3-methyl-2-oxo-7-oxabicyclo[4.1.0]hept-3-yl]octahydro-1h-indene-1-carboxylate (iii) (1s,2s)-2-aminocyclopentanol (i) (2r,3r,4r,5r)-4-(acetoxy)-2-[(acetoxy)methyl]-5-(6-[[(1s,2s)-2-hydroxycyclopentyl]amino]-9h-purin-9-yl)tetrahydro-3-furanyl acetate (ii) Reference 1:     griss, g.; et al. (boehringer ingelheim gmbh); 2-amino-4,5,7,8-tetrahydro-6h-thiazolo or oxazolo[5,4-d]azepines and salts. es 396454; fr 2102192; gb 1321509; nl 7111176; us 3804849 . Reference 2:     serradell, m.n.; blancafort, p.; castaner, j.; thorpe, p.j.; b-ht-920. drugs fut 1980, 5, 10, 481.

來源:藥化網

作者:藥化小編

摘要:本文合成路線介紹的是藥物中文名鹽酸他利克索；英文名Talipexole dihydrochloride;BHT-920;B-HT-920;Domin；CAS[36085-73-1]

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