1070955-54-2

Upstream product

• 194979-77-6 tert-butyl 2-oxo-1,2,3,4-tetrahydroquinoline-1-carboxylate 
• 1224967-99-0 C₁₄H₁₇NO₄ 

Downstream Products

• 1154703-35-1 3-(2-t-butoxycarbonylaminophenyl)propionic acid 2-(11,17-dihydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2-oxo-ethyl ester 
• 1233497-38-5 (2-{3-oxo-3-[4-(5-p-tolyl-3-trifluoromethyl-pyrazol-1-yl)-benzenesulfonylamino]-propyl}-phenyl)-carbamic acid tert-butyl ester 
• 1314005-13-4 3-(2-(tert-butoxycarbonylamino)phenyl)propionic acid 2-(11,17-dihydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl ester 

Relevant academic research and scientific papers

Intramolecular aldol reaction of N-Acylated (2-Aminophenyl)-α- oxoacetic Acids: Rapid access to Tri- and tetracyclic 1,2-dihydroquinolin-2(1 H)-ones

A four-step synthesis of tri- and tetracyclic 1,2-dihydroquinolin-2(1H)- ones via acylation of various substituted isatins with readily available N-Boc-protected aminoacids followed by an intramolecular aldol reaction and cyclization has been developed. The final products were obtained in moderate to excellent overall yields.

Design, synthesis, and pharmacological effects of a cyclization-activated steroid prodrug for colon targeting in inflammatory bowel disease

Glucocorticoids are used in the treatment of inflammatory bowel disease. A limitation to their use is that they undergo absorption from the GIT before reaching the colon causing severe systemic side effects. We report here on a novel prodrug approach to targeting corticosteroids to the colon. The design involves attaching a 21-ester group that suppresses absorption during transit to the colon. The prodrug is designed to be primed by colonic microflora liberating an amino ester that cyclizes releasing the steroid. One of the prodrugs 5b was as efficacious as prednisolone in the murine DSS model but did not cause thymic atrophy, a marker for systemic steroid effects.

Microwave-assisted N-Boc deprotection under mild basic conditions using K3PO4·H2O in MeOH

A simple and efficient method for the deprotection of secondary Boc-protected amino compounds under mild basic conditions using K3PO4·H2O in MeOH assisted by microwave irradiation has been presented.