109554-51-0

Upstream product

• 28744-77-6 sodium diethyl-2-phenylmalonate 
• 105-36-2 ethyl bromoacetate 
• 607-81-8 diethyl 2-benzylmalonate 
• 7459-46-3 triethyl 1,1,2-ethanetricarboxylate 
• 100-44-7 benzyl chloride 
• 105-39-5 chloroacetic acid ethyl ester 
• 996-82-7 sodium diethylmalonate 

Downstream Products

• 36092-42-9 2-benzylsuccinic acid 
• 3033-50-9 3-phenyl-1,1,2-propanetricarboxylic acid 1,1,2-triethyl ester 
• 6566-40-1 4-oxo-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid 
• 19544-43-5 3-benzyldihydrofuran-2,5-dione 
• 856061-15-9 (4-benzyl-3,5-dioxo-pyrazolidin-4-yl)-acetyl azide 

Relevant academic research and scientific papers

Synthesis of optically active α-benzyl paraconic acids and their esters and assignment of their absolute configuration

The cis- and trans-4-benzylparaconic acids and their ethyl esters were synthesized with high enantiomeric excess by hydrolysis of the corresponding diastereomeric lactonic esters using α-chymotrypsin. Thus, at low conversion values, cis- and trans-4-benzyl-5-oxo-3-tetrahydrofurancarboxylic acids were separately isolated with 99% ee and 92% ee, respectively. Both ethyl ester diastereomers were also obtained in enantiopure form. The absolute configuration of the trans-lactonic acid was assigned by 1H NMR analysis of its ester derivatives with both enantiomers of 1-(9-anthryl)-2,2,2-trifluoroethanol, while that of the cis-lactonic acid was assigned by means of X-ray analysis of a crystalline derivative. The circular dichroism curves of the products obtained are also reported.

2-Amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors

Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hy

Novel compounds

Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: wherein X and Y are selected independently from hydrogen and aryl, which aryl is unsubstituted or substituted one or more times by hydroxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aryl, heterocyclyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkoxy, C1-6alkyl, C1-6alkoxy or halo, which alkyl or alkoxy groups are unsubstituted or substituted one or more times by halo; m and n are independently 0 to 3, provided that m and n are not both 0; A represents a single bond or is —(CRpa Rpb)p— wherein p is 1-3 and Rpa and Rpb are selected independently from hydrogen, C1-6alkyl, C1-6alkoxy and halo, which alkyl or alkoxy groups are independently substituted one or more times by halo; B represents a C4-8 saturated or unsaturated ring, which ring is unsubstituted or substituted one or more times by C1-6alkyl, C1-6alkoxy, aryl, aryloxy, hydroxy, oxo, halo, amino, C1-6alkylamino, di(C1-6 alkyl)amino, and C1-6alkylamido, which C1-6alkyl or C1-6alkoxy groups are unsubstituted or substituted one or more times by halo, which aryl group is unsubstituted or substituted one or more times by aryl, heterocyclyl, aryloxy, arylC1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkyl, hydroxy, C1-6alkenoxy, C1-6alkoxy, halo, or C1-6alkyl, which C1-6alkyl may be substituted one or more times by halo, and which aryl group is linked to said ring by a single bond or is benzo-condensed therewith are ligands of the ORL-1 receptor.

Therapeutic substituted indole compounds and compositions thereof

The present invention is concerned with compounds of formula (I) STR1 wherein R, R1 and R2 are independently selected from hydrogen and C1-4 alkyl; R3 and R4 are independently selected from hydrogen, C1-6 alkyl (including cycloalkyl) and aryl (wherein the alkyl or aryl group, which latter includes benzyl, is optionally substituted by one or more atoms or groups independently selected from halogen, C1-4 alkyl and aryl), provided R3 benzyl or substituted benzyl when R4 =H; m is an integer of from 0 to 2; n is an integer of from 0 to 3; (W) is a group of formula (i), (ii), (iii), or (iv) STR2 wherein Y is selected from oxygen, methylene and >N--R5, where R5 is hydrogen, C1-4 alkyl, or benzyl, Z and Z' are independently selected from >C=O, >C=S and methylene, and the chiral center * in formula (i) or (ii) is in its (S) or (R) form or is a mixture thereof in any proportions; X is a group selected from aryl (including heteroaryl) xanthenyl dibenzofuranyl which group is optionally substituted; and salts and solvates thereof, the preparation of these compounds, pharmaceutical formulations containing them and their use in medicine, particularly in the treatment of migraine.