127510-92-3

Upstream product

• 1128-76-3 3-chloro-benzoic acid ethyl ester 
• 19158-51-1 P-toluenesulfonyl cyanide 
• 6388-47-2 2-amino-3-chlorobenzoic acid 
• 269738-15-0 ethyl 2-amino-3-chlorobenzoate 

Downstream Products

• 918402-80-9 4-chloro-3-cyano-phthalic acid diethyl ester 
• 918402-81-0 5-chloro-4-cyano-benzene-1,2,3-tricarboxylic acid triethyl ester 
• 1254073-93-2 3-chloro-2-cyanobenzoic acid 
• 1261849-80-2 2-chloro-6-(hydroxymethyl)benzonitrile 

Relevant academic research and scientific papers

Compounds Useful as Immunomodulators

The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6 R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.

Highly functionalized benzene syntheses by directed mono or multiple magnesiations with TMPMgCl·LiCl

The direct magnesiation of highly functionalized aromatics bearing an ester, a nitrile, or a ketone can be readily performed by using an OBoc as a directing group and TMPMgCl·LiCl as a base. It allows, for example, the preparation of a meta-magnesiated benzophenone in >95%. After quenching, highly functionalized and substituted benzenes are obtained.