CAS 352-11-4

alpha-Chloro-4-fluorotoluene1-(Chloromethyl)-4-fluorobenzene

Codes: Mosapride Citrate-030

Application context (from source-drug indications)

GastritisMosapride CitrateEnteral feeding intoleranceMosapride CitrateIrritable bowel syndromeMosapride CitrateDyspepsiaMosapride CitrateConstipationMosapride Citrate

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Mosapride Citrate	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.

Mosapride CitrateOptimised routesteps: 6total yield: /

[4-(4-Fluorobenzyl)-2-morpholinyl]methylamine→2-Hydroxyethylamine→2-[[(4-Fluorophenyl)methyl]amino]ethan-1-ol→1,3-Dihydro-1,3-dioxoisoindole potassium salt→Glycerol-alpha,gamma-dichlorohydrin→N-(3-Chloro-2-hydroxypropyl)-phthalimide→2-(3-[[(4-Fluorophenyl)methyl](2-hydroxyethyl)amino]-2-hydroxypropyl)-1H-isoindole-1,3(2H)-dione→2-[2-Hydroxy-3-[(2-hydroxyethyl)amino]propyl]-1H-isoindole-1,3(2H)-dione→Morpholin-2-ylmethanamine→alpha-Chloro-4-fluorotoluene

Mosapride CitrateOptimised routesteps: 4total yield: /

[(2R)-4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl phenylmethanesulfonate→(2R)-2-(Phenylmethoxymethyl)oxirane→Sodium (2-aminoethyl) sulfate→2(R)-(Benzyloxymethyl)morpholine→(2R)-morpholin-2-ylmethanol→1-(Chloromethyl)-4-fluorobenzene→{4-[(4-fluorophenyl)methyl]morpholin-2-yl}methyl 4-methylbenzene-1-sulfonate

Mosapride CitrateProcess routesteps: 4total yield: 363g(Mosapride Citrate (API))

Morpholin-2-ylmethanamine→4-Amino-5-chloro-2-ethoxybenzoic acid→4-Amino-5-chloro-2-ethoxy-N-(morpholin-2-ylmethyl)benzamide→4-Acetamido-5-chloro-2-ethoxy-N-[(morpholin-2-yl)methyl]benzamide→1-(Chloromethyl)-4-fluorobenzene→4-Acetamido-5-chloro-2-ethoxy-N-([4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl)benzamide

Intermediates available on this site

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