CAS 186204-35-3

((1R,2R)-cyclohexane-1,2-diyl)bis(methylene) dimethanesulfonate

Codes：LURA-003、LURA-017

Application context (from source-drug indications)

重度抑郁症盐酸鲁拉西酮精神分裂症盐酸鲁拉西酮躁狂症盐酸鲁拉西酮抑郁症盐酸鲁拉西酮

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
盐酸鲁拉西酮Lurasidone Hydrochloride	Tier B — Position early	2028

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.

盐酸鲁拉西酮原研路线steps: 4total yield: /

3-(piperazin-1-yl)benzo[d]isothiazole→(3aR,7aR)-4'-(benzo[d]isothiazol-3-yl)octahydrospiro[isoindole-2,1'-piperazin]-2-ium methanesulfonate→(3aR,4S,7R,7aS)-hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione→(3aR,7aR)-hexahydroisobenzofuran-1,3-dione→((1R,2R)-cyclohexane-1,2-diyl)dimethanol→((1R,2R)-cyclohexane-1,2-diyl)bis(methylene) dimethanesulfonate

盐酸鲁拉西酮优化路线steps: 5total yield: /

(3aR,4S,7R,7aS)-hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione→((1R,2R)-cyclohexane-1,2-diyl)bis(methylene) dimethanesulfonate→2,2'-azanediylbis(ethan-1-ol)→((1R,2R)-2-((bis(2-hydroxyethyl)amino)methyl)cyclohexyl)methyl methanesulfonate→(3aR,4S,7R,7aS)-2-(((1R,2R)-2-((bis(2-hydroxyethyl)amino)methyl)cyclohexyl)methyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione→((((1R,2R)-2-(((3aR,4S,7R,7aS)-1,3-dioxooctahydro-2H-4,7-methanoisoindol-2-yl)methyl)cyclohexyl)methyl)azanediyl)bis(ethane-2,1-diyl) dimethanesulfonate→benzo[d]isothiazol-3-amine

盐酸鲁拉西酮优化路线steps: 3total yield: 4.5 g

3-(piperazin-1-yl)benzo[d]isothiazole→(3aR,7aR)-4'-(benzo[d]isothiazol-3-yl)octahydrospiro[isoindole-2,1'-piperazin]-2-ium methanesulfonate→(3aR,4S,7R,7aS)-hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione→((1R,2R)-cyclohexane-1,2-diyl)bis(methylene) dimethanesulfonate

Intermediates available on this site

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Supplier	Product	Price band	MOQ	Lead time	Qualifications
Unibest Nantong cGMP Site	(R,R)-1,2-bis(methanesulfonyloxymethyl)cyclohexane Pharmaceutical Intermediates	询价	询价	询价	—

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