129689-07-2

Upstream product

• 108-59-8 malonic acid dimethyl ester 
• 88-65-3 2-bromobenzoic-acid 
• 1148132-51-7 2-[(2-benzyloxycarbonyl)phenyl]malonic acid dimethyl ester 

Downstream Products

• 1148131-32-1 2-(2-formylphenyl)malonic acid dimethyl ester 
• 1416767-40-2 dimethyl 1,1-dibenzyl-6-oxo-1,3,4,11a-tetrahydro-2H-pyrido[1,2-b]isoquinoline-11,11(6H)-dicarboxylate 
• 137643-12-0 [2-(4-Bromo-2-fluoro-benzyl)-1,3-dioxo-1,2,3,4-tetrahydro-isoquinolin-4-yl]-acetic acid tert-butyl ester 
• 133891-92-6 2-[(4-bromo-2-fluorophenyl)methyl]-1,2,3,4-tetrahydro-1,3-dioxo-4-isoquinolineacetic acid 
• 137643-14-2 2-(4-Bromo-2-fluoro-benzyl)-4-chlorocarbonylmethyl-1,3-dioxo-1,2,3,4-tetrahydro-isoquinoline-4-carboxylic acid methyl ester 
• 129688-82-0 2-<(4-bromo-2-fluorophenyl)methyl>-1,2,3,4-tetrahydro-4-(methoxycarbonyl)-1,3-dioxo-4-isoquinolineacetic acid 
• 129688-94-4 4-(2-amino-2-oxoethyl)-2-<(4-bromo-2-fluorophenyl)methyl>-1,2,3,4-tetrahydro-4-(methoxycarbonyl)-1,3-dioxo-4-isoquinolineacetic acid methyl ester 
• 129688-76-2 2-[(4-Bromo-2-fluorophenyl)methyl]-1,2,3,4-tetrahydro-4-(methoxycarbonyl)-1,3-dioxo-4-isoquinolineacetic Acid 1,1-Dimethylethyl Ester 
• 142371-22-0 2-<(4-bromo-2-fluorophenyl)methyl>-4-(cyanomethyl)-1,2,3,4-tetrahydro-1,3-dioxo-4-isoquinolinecarboxylic acid methyl ester 
• 129688-70-6 2-[(4-Bromo-2-fluorophenyl)methyl]-1,2,3,4-tetrahydro-1,3-dioxo-4-isoquinoline-carboxylic Acid Methyl Ester 
• 137643-17-5 2-(2-Chlorocarbonyl-phenyl)-malonic acid dimethyl ester 

Relevant academic research and scientific papers

Formation of carbocycles by intramolecular conjugate displacement: Scopeand mechanistic insights

A detailed study has been made of a method of ring closure categorized as an all-carbon intramolecular conjugate displacement (ICD). This reaction involves intramolecular addition of a carbanion, which is stabilized by at least one electron-withdrawing group, to a Michael acceptor which has a leaving group in an allylic position. The process formally resembles a combination of Michael addition and S N2' displacement. The overall result is formation of a ring with loss of the allylic leaving group and shift of the original double bond to a new location spanning the positions of the electron-withdrawing substituent of the Michael acceptor subunit and the original allylic leaving group. The starting materials are easily prepared by a selenium-based version of the Morita-Baylis-Hillman reaction. The cyclizations are transition metal free and occur under mild conditions, using DBU or Cs 2CO 3 inMeCN or THF. Acetate is a suitable leaving group and the electron-withd rawing substituent of the Michael acceptor unit can be CO 2R,SO 2Ph, or CN. Six- and seven-membered rings are formed effi ciently, and complex structures, such as those resembling the core of CP-225,917, are easily assembled. The products of these ICD reactions are themselves classical Michael acceptors. A range of mechanisms probably operates, depending on the structure of the starting material and the reaction conditions, but conclusive evidence for a stepwise mechanism was obtained in a suitably biased case, while other observations are compatible with a concerted process or a stepwise path involving a short-lived carbanion that evades capture by a proton source.

Facile synthesis of novel spiro[azetidine-2,4'(1H)-isoquinoline-1',3',4(2'H)-triones]

A convenient general method for the synthesis of a new heterocycle, spiro[azetidine-2,4'(1'H)-isoquinoline-1',3',4(2'H)-trione] is described. The key intermediate 2 was prepared by direct halogenation of position-4 of acid 3 with thionyl chloride, and sub

Novel spirosuccinimide aldose reductase inhibitors derived from isoquinoline-1,3-diones: 2-[(4-Bromo-2-fluorophenyl)methyl]-6- fluorospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrone and congeners. 1

The high concentrations of plasma glucose formed during diabetic hyperglycemia rapidly translate into high levels of glucose in tissues where glucose uptake is independent of insulin. In these tissues that include the lens, retina, nerve, and kidney, this

ISOQUINOLINE-1,3-DIONE ACETYL CARBAMATES USEFUL AS ALDOSE REDUCTASE INHIBITORS

This invention relates to isoquinoline-1,3-dione acetyl carbamates and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have

Alkylidene analogs of 1'-amino-2-[(benzothiazolyl)-methyl]spiro [isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones useful as aldose reductase inhibitors

This invention relates to alkylidene analogs of 1'-amino-2-[(benzothiazolyl)-methyl]spiro[isoquinoline-4(1H),3'-pyrrolidone]-1,2',3,5'(2H)-tetrones represented by formula (I): STR1 wherein: R1, R2 and R3 are independently

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF SPIRO(ISOQUINOLINE-4(1H), 3'-PYRROLIDINE)-1,2',3,5'(2H)-TETRONES WHICH ARE USEFUL AS ALDOSE REDUCTASE INHIBITORS

The invention relates to a process for producing spiroisoquinoline pyrrolidines. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.

SPIRO-PYRIDAZINES AND ANALOGS THEREOF USEFUL AS ALDOSE REDUCTASE INHIBITORS

This invention relates to spiro-pyridazines, to processes for their preparation, to methods for using the compounds, and to pharmaceutical prepartions thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or

SPIRO-LACTAMS AND ANALOGS THEREOF USEFUL AS ALDOSE REDUCTASE INHIBITORS

This invention relates to spiro-lactams and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties w

1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones and analogs thereof useful as aldose reductase inhibitors

This invention relates to 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones of structural formula (I) STR1 wherein: R1 and R2 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, halogen, lower alko

SPIRO-ISOQUINOLINE-PYRROLIDINES AND ANALOGS THEREOF USEFUL AS ALDOSE REDUCTASE INHIBITORS

This invention relates to spiro-isoquinoline-pyrrolidines and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceu