78184-72-2

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 63701-55-3 (R)-(-)-baclofen hydrochloride 
• 91837-43-3 1,3-dioxoisoindolin-2-yl (tert-butoxycarbonyl)glycinate 
• 919349-69-2 (S)-5-(tert-Butyl-diphenyl-silanyloxymethyl)-2-oxo-3-phenylselanyl-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 144564-15-8 4R,5S-1-t-butoxycarbonyl-5-t-butyldiphenylsiloxymethyl-4-(4-chlorphenyl)pyrrolidine-2-one 
• 144564-10-3 2S,3R-1-t-butoxycarbonyl-3-(4-chlorophenyl)-5-oxo-pyrrolidine-2-carboxylic acid 
• 144564-09-0 4R,5S-1-t-butoxycarbonyl-4-(4-chlorophenyl)-5-hydroxymethyl-pyrrolidine-2-one 
• 873-77-8 (4-chlorphenyl)magnesium bromide 
• 138629-30-8 (S)-tert-butyl 2-((tert-butyldiphenylsilyloxy)methyl)-5-oxopyrrolidine-1-carboxylate 
• 138871-58-6 (S)-2-(tert-butyl-diphenyl-silanyloxymethyl)-5-oxo-2,5-dihydro-pyrrole-1-carboxylic acid tert-butyl ester 
• 1095545-18-8 (3R)-3-(4-chlorophenyl)pyrrolidine hydrochloride 
• 171897-39-5 (R)-tert-butyl 3-(4-chlorophenyl)pyrrolidine-1-carboxylate 
• 144564-11-4 (R)-tert-butyl 4-(4-chlorophenyl)-2-oxopyrrolidine-1-carboxylate 

Downstream Products

• 63701-55-3 (R)-(-)-baclofen hydrochloride 
• 847352-39-0 benzyl 4-tert-butoxycarbonylamino-(3R)-(4-chlorophenyl)butanoate 

Relevant academic research and scientific papers

Synthesis of β-Substituted γ-Aminobutyric Acid Derivatives through Enantioselective Photoredox Catalysis

β-Substituted chiral γ-aminobutyric acids feature important biological activities and are valuable intermediates for the synthesis of pharmaceuticals. Herein, an efficient catalytic enantioselective approach for the synthesis of β-substituted γ-aminobutyr

ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE

The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof , methods of making prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±) 4 amino 3 (4 chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

Stereospecific synthesis of (R)- and (S)-Baclofen and (R)- and (S)- PCPGABA [4-amino-2-(4-chlorophenyl)butyric acid] via (R)- and (S)-3-(4- chlorophenyl)pyrrolidines

(R)- and (S)-baclofen and (R)- and (S)-PCPGABA [4-amino-2-(4- chlorophenyl)butyric acid] were stereospecifically synthesized via (R)- and (S)-3-(4-chlorophenyl)pyrrolidines, starting from trans-4-hydroxy-L-proline. The syntheses involve two key operations

Synthesis of Homochiral R-Baclofen from S-Glutamic Acid

A streoselective synthesis of R-Baclofen is presented starting from S-pyroglutamic acid derivative 3.The key steps are the 1,4-conjugate addition of Grignard cuprate (p-ClPh)2CuMgCl to 3 and Barton-Decarboxylation of 6e to 7e.