CAS 124-40-3

dimethylamineDimethylamine

Codes：RIBO-007、DESV-002、Desvenlafaxine-012

Application context (from source-drug indications)

乳腺癌琥珀酸瑞波西利抑郁症琥珀酸去甲文拉法辛重度抑郁症琥珀酸去甲文拉法辛抑郁琥珀酸去甲文拉法辛糖尿病神经病变琥珀酸去甲文拉法辛疼痛琥珀酸去甲文拉法辛纤维肌痛琥珀酸去甲文拉法辛重度抑郁症地文拉法辛抑郁症地文拉法辛

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
琥珀酸瑞波西利Ribociclib Succinate	Tier A — Act now	2029
琥珀酸去甲文拉法辛Desvenlafaxine Succinate Hydrate	Tier C — Watch / trade	-
地文拉法辛Desvenlafaxine	Tier C — Watch / trade	-

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.

琥珀酸瑞波西利原研路线steps: 9total yield: 45.7 g

5-bromo-2,4-dichloropyrimidine→cyclopentanamine→5-bromo-2-chloro-N-cyclopentylpyrimidin-4-amine→prop-2-yn-1-ol→3-(2-chloro-4-(cyclopentylamino)pyrimidin-5-yl)prop-2-yn-1-ol→(2-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)methanol→dimethylamine→2-chloro-7-cyclopentyl-N,N-dimethyl-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide→tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate→tert-butyl 4-(6-((7-cyclopentyl-6-(dimethylcarbamoyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate→5-chloro-2-nitropyridine→piperazine→1-(6-nitropyridin-3-yl)piperazine→tert-butyl 4-(6-nitropyridin-3-yl)piperazine-1-carboxylate

琥珀酸去甲文拉法辛原研路线steps: 5total yield: 325 g

2-(4-methoxyphenyl)acetic acid→dimethylamine→2-(4-methoxyphenyl)-N,N-dimethylacetamide→2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl)-N,N-dimethylacetamide→DESV-005→4-(2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl)phenol

地文拉法辛优化路线steps: 7total yield: 5.8g(Desvenlafaxine (Free))

2-(4-Hydroxyphenyl)acetic acid→2-(4-Hydroxyphenyl)acetyl chloride→Dimethylamine→2-(4-Hydroxyphenyl)-N,N-dimethylacetamide→2-[4-[tert-Butyl(dimethyl)silyloxy]phenyl]-N,N-dimethylacetamide→Cyclohexanone→2-[4-[tert-Butyl(dimethyl)silyloxy]phenyl]-2-(1-hydroxycyclohexyl)-N,N-dimethylacetamide→4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol→2-(1-Hydroxycyclohexyl)-2-(4-hydroxyphenyl)-N,N-dimethylacetamide

地文拉法辛优化路线steps: 8total yield: 5.13g(Desvenlafaxine succinate (API))

1-(4-Hydroxyphenyl)ethanone→1-[4-(Benzyloxy)phenyl]ethanone→1-[4-(benzyloxy)phenyl]-2-bromoethan-1-one→Dimethylamine→1-[4-(Benzyloxy)phenyl]-2-(dimethylamino)ethanone hydrobromide→1-[4-(Benzyloxy)phenyl]-2-(dimethylamino)ethanol hydrochloride→2-[4-(Benzyloxy)phenyl]-2-chloro-N,N-dimethylethanamine hydrochloride→Cyclohexanone→1-{1-[4-(Benzyloxy)phenyl]-2-(dimethylamino)ethyl}cyclohexan-1-ol→4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol

Intermediates available on this site

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Supplier	Product	Price band	MOQ	Lead time	Qualifications
Unibest Nantong cGMP Site	2-Chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid Pharmaceutical Intermediates	询价	询价	询价	—
Unibest Taizhou GMP-like Site	2-Chloro-7-cyclopentyl-N,N-dimethyl-7H-pyrrolo[2,3-d]pyrimidine-6- carboxamide Pharmaceutical Intermediates	询价	询价	询价	—

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