1030837-74-1

Basic information

• Product Name: Tert-butyl (2R)-2-[(1R)-(4-Chloro-2-methoxy-phenoxy)-phenyl-methyl]-morpholine-4-carboxylate
• Synonyms: Tert-butyl (2R)-2-[(1R)-(4-Chloro-2-methoxy-phenoxy)-phenyl-methyl]-morpholine-4-carboxylate
• CAS NO: 1030837-74-1
• Molecular Weight: 433.932
• Mol File: 1030837-74-1.mol

Chemical Properties

• CAS DataBase Reference: Tert-butyl (2R)-2-[(1R)-(4-Chloro-2-methoxy-phenoxy)-phenyl-methyl]-morpholine-4-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: Tert-butyl (2R)-2-[(1R)-(4-Chloro-2-methoxy-phenoxy)-phenyl-methyl]-morpholine-4-carboxylate(1030837-74-1)
• EPA Substance Registry System: Tert-butyl (2R)-2-[(1R)-(4-Chloro-2-methoxy-phenoxy)-phenyl-methyl]-morpholine-4-carboxylate(1030837-74-1)

Safety Data

• Hazardous Substances Data: 1030837-74-1(Hazardous Substances Data)

Upstream product

• 1030837-66-1 C₁₇H₂₅NO₆S 
• 16766-30-6 4-Chloroguaiacol 

Downstream Products

• 869183-47-1 (2R)-2-[(1R)-(4-chloro-2-methoxyphenoxy)(phenyl)methyl]morpholine 
• 869208-83-3 (2R)-2-[(1R)-(4-chloro-2-methoxyphenoxy)(phenyl)methyl]morpholine succinate 

Relevant articles and documents

Enantioselective synthesis of (R)- and (S)-N-Boc-morpholine-2-carboxylic acids by enzyme-catalyzed kinetic resolution: application to the synthesis of reboxetine analogs

The (R)- and (S)-N-Boc-morpholine-2-carboxylic acids 9 and 10 were prepared using an enantioselective synthesis employing a highly selective enzyme-catalyzed kinetic resolution of racemic n-butyl 4-benzylmorpholine-2-carboxylate (11) as the key step. Acids 9 and 10 were then converted efficiently and stereoselectively to reboxetine analogs 3 and 4.

Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition

Single enantiomer (SS) and (RR) 2-[(phenoxy)(phenyl)methyl]morpholine derivatives 5, 8-23 are inhibitors of monoamine reuptake. Target compounds were prepared using an enantioselective synthesis employing a highly specific enzyme-catalysed resolution of racemic n-butyl 4-benzylmorpholine-2-carboxylate (26) as the key step. Structure-activity relationships established that serotonin and noradrenaline reuptake inhibition are functions of stereochemistry and aryl/aryloxy ring substitution. Consequently, selective SRI, selective NRI and dual SNRIs were all identified. One of these compounds, a potent and selective dual SNRI, (SS)-5a was selected as a candidate for further pre-clinical evaluation.

Novel compounds

The present invention provides compounds of Formula I wherein R1, R2, R3, and n have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment