98581-93-2

Usage

InChI:InChI=1/C9H8Cl2O/c10-8-4-3-7(2-1-5-12)9(11)6-8/h3-6H,1-2H2

Upstream product

• 29898-32-6 2,4-dichloro-1-iodo-benzene 
• 107-18-6 allyl alcohol 
• 146882-07-7 3-(2,4-dichlorophenyl)propan-1-ol 
• 69793-07-3 ethyl 3-(2,4-dichlorophenyl)propanoate 
• 20595-45-3 2,4-dichlorocinnamic acid 

Downstream Products

• 848081-12-9 2-amino-5-(2',4'-dichlorobenzyl)thiophene-3-carboxylic acid ethyl ester 
• 70017-27-5 3-(2,4-Dichlorophenyl)propenal 
• 1394046-58-2 (R)-2-(2,4-dichlorobenzyl)-5-oxohexanal 

Relevant academic research and scientific papers

Synthesis of optically active 4-substituted 2-cyclohexenones

Recently, Nicolaou and Baran independently synthesized optically active 4-substituted 2-cyclohexenones via an efficient LiOH-mediated intramolecular aldol condensation. Thus far, application of their cyclization approach has been limited to ketoaldehydes where the R-group is branched. It is demonstrated that the LiOH-mediated cyclization, when applied to substrates containing unbranched R-groups, results in significant erosion of optical purity. A mechanistic justification is provided, and a set of neutral, organocatalyzed conditions is identified that enables cyclization with little loss in optical purity.

6-HYDROXY-DIBENZODIAZEPINONES USEFUL AS HEPATITIS C VIRUS INHIBITORS

Inhibitors of HCV replication of formula (I) the stereoisomers, prodrugs, tautomers, racemics, salts, hydrates or solvates thereof wherein R1, R2; R3; R4a and R4b have the meaning defined in the claims.The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.

DIBENZODIAZEPINONES USEFUL AS HEPATITIS C VIRUS INHIBITORS

Inhibitors of HCV replication of formula (I) and the stereoisomers, prodrugs, tautomers, racemics, salts, hydrates or solvates thereof, wherein X, Y, R1; R2; R3; R4a and R4b have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.

5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES

The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I),wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.

7-PHENYL-ISOQUINOLINE-5-SULFONYLAMINO DERIVATIVES AS INHIBITORS OF AKT (PROTEINKINASE B)

The present invention relates to compounds Formula (I) as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.

Synthesis of classical and nonclassical 2-amino-4-oxo-6-benzylthieno-[2,3- d]pyrimidines as potential thymidylate synthase inhibitors

A series of seven nonclassical 2-amino-4-oxo-6-substituted thieno[2,3-d]pyrimidines 2-8 and one classical N-[4-(2-amino-4-oxo-3,4- dihydrothieno[2,3-d]pyrimidin-6-ylmethyl)benzoyl]-L-glutamic acid 9 (Table I) were designed as the first in a series of 6-substituted 6-5 fused ring analogs as potential thymidylate synthase (TS) inhibitors and as antitumor agents. The target compounds were synthesized via a Heck coupling of appropriately substituted iodobenzenes and allyl alcohol followed by cyclization using cyanoacetate and sulfur powder to afford substituted thiophenes. The resulting thiophenes were then cyclocondensed with chloroformamidine hydrochloride to afford 2-amino-4-oxo-6-substituted thieno[2,3-d]pyrimidines 2-8 and 26. Hydrolysis of 26 followed by coupling with diethyl L-glutamate afforded 28. The classical analog 9 was obtained by hydrolysis of 28. None of the target compounds inhibited human recombinant thymidylate synthase at 23 μM except 9 for which the IC50 value was 100 μM.