112733-45-6

Upstream product

• 75-44-5 phosgene 
• 112733-54-7 ethyl N-(2-carbamoyl-5-chlorophenyl)aminoacetate 
• 75158-06-4 N-(2-carbamoyl-5-chlorophenyl)aminoacetate 
• 13165-35-0 7-chloroquinazoline-2,4-dione 
• 105-36-2 ethyl bromoacetate 
• 89-77-0 2-Amino-4-chlorobenzoic acid 
• 214288-97-8 4-chloro-2-ureido-benzoic acid 
• 105-39-5 chloroacetic acid ethyl ester 

Downstream Products

• 112733-28-5 ethyl 2-[3-(4-bromo-2-fluorobenzyl)-7-chloro-1,2,3,4-tetrahydro-2,4-dioxoquinazoline-1-yl)acetate 
• 112733-06-9 zenarestat 

Relevant academic research and scientific papers

The process development of a novel aldose reductase inhibitor, FK366. Part 1. Improvement of discovery process and new syntheses of 1-substituted quinazolinediones

This contribution describes part 1 of process development of a novel aldose reductase inhibitor FK366 (1). The original process applied on a laboratory scale was improved from the safety viewpoint to manufacture materials on 500-L scale suitable for toxic

Process for producing quinazoline derivatives

This invention provides an industrially useful process for producing a quinazoline derivative (I) of the general formula: [wherein R1is hydrogen or halogen; R2is carboxy or protected carboxy; A is lower alkylene] or its salt on a commercial scale which comprises reacting a compound of the general formula: [wherein R1is hydrogen or halogen] or its salt with a silylating agent and then with a compound of the general formula: Cl—A—R2??(III) [wherein R2 is carboxy or protected carboxy; A is lower alkylene] or its salt, optionally followed by desilylation.

Process for producing quinazoline derivatives

A process for producing 1,2,3,4-tetrahydro-2,4-dioxo-quinazoline-1-yl acetic acid derivatives of the formula (I) in which R1, R2, R3 and R4 are mutually independently hydrogen, halogen, OH, NO2, (C1 -C6) alkoxy, (C1 -C6) alkyl, halogen-substituted (C1 -C6) alkyl, R5 is hydrogen, (C1 -C6) alkyl, phenyl where the alkyl or phenyl radical may also be substituted by halogen atoms; in which an anthranilic acid derivative of formula (II), in which R1 to R5 have the above meaning and R6 is hydrogen, (C1 -C6) alkyl or phenyl, where the alkyl or phenyl radical may also be substituted by halogen atoms, is reacted with a metal cyanate and hydrogen chloride in the presence of an inert solvent. STR1

Process for producing dioxoquinazolines

A process for producing an dioxoquinazoline of following formula (II): STR1 wherein R1 and R2 independently represent a hydrogen atom, a halogen atom, a nitro group, a lower alkyl group, an aralkyl group, an alkoxy group, an alkoxylcarbonyl group or a group represented by YNR3 R4, wherein Y represents a direct bond, a lower alkylene group or a carbonyl group, and R3 and R4 independently represent a lower alkyl group or N, R3 and R4 may bond together to form a five- or six-membered heterocycle which comprises reacting an anthranylamide of formula (I): STR2 wherein X, R1 and R2 are as defined above.

Quinazoline derivatives, compositions thereof and their use in treating diabetic complications

The invention relates to compounds of the formula: STR1 in which R1 and R2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl, R3 is dihalophenyl, naphthyl(lower)alkyl, phenyl(lower)alkyl substituted by one or two substituent(s) selected from the group consisting of halogen, lower alkoxy, halo(lower)alkyl and lower alkyl, or thienyl(lower)alkyl, R4 is carboxy or protected carboxy, Y is carbonyl, thiocarbonyl or sulfonyl and Z is lower alkylene, and pharmaceutically acceptable salts thereof, useful in the treatment of diabetic complications.