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CAS 18621-18-6

azetidin-3-ol hydrochloride

Codes:DELAF-005、COBI-001

Application context (from source-drug indications)

社区获得性细菌肺炎德拉沙星社区获得性肺炎德拉沙星细菌性皮肤疾病德拉沙星皮肤和皮肤结构感染德拉沙星黑色素瘤可美替尼

Source drugs (routes using this intermediate)

DrugTierExpiry
德拉沙星DelafloxacinTier C — Watch / trade2029
可美替尼Cobimetinib FumarateTier C — Watch / trade2029

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

德拉沙星原研路线steps: 4total yield: 73 kg
2,4,5-trifluorobenzoic acid→ethyl 3-oxo-3-(2,4,5-trifluorophenyl)propanoate→3,5-difluoropyridine-2,6-diamine→(Z)-ethyl 3-((6-amino-3,5-difluoropyridin-2-yl)amino)-2-(2,4,5-trifluorobenzoyl)acrylate→azetidin-3-ol hydrochloride→ethyl 1-(6-amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-(isobutyryloxy)azetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate
德拉沙星优化路线steps: 6total yield: 3.0 g
3,5-difluoropyridine-2,6-diamine→azetidin-3-ol hydrochloride→ethyl 3-(3-chloro-2,4,5-trifluorophenyl)-3-oxopropanoate→(Z)-ethyl 2-(3-chloro-2,4,5-trifluorobenzoyl)-3-ethoxyacrylate→(Z)-ethyl 3-((6-amino-3,5-difluoropyridin-2-yl)amino)-2-(3-chloro-2,4,5-trifluorobenzoyl)acrylate→ethyl 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate→ethyl 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate→sodium 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate

Intermediates available on this site

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