16216-94-7

Upstream product

• 67-56-1 methanol 
• 4476-28-2 (4-isopropylphenyl)acetic acid 
• 75633-89-5 1-(2,2-difluoroethenyl)-4-isopropylbenzene 
• 645-13-6 4-isopropylacetophenone 

Downstream Products

• 4476-28-2 (4-isopropylphenyl)acetic acid 
• 52629-44-4 4-(1-methylethyl)-benzeneacetyl chloride 
• 1267356-14-8 C₁₄H₁₈O₄ 
• 195070-89-4 methyl 2-(4-isopropylphenyl)-2-oxoacetate 
• 131602-93-2 2-(4-Isopropyl-phenyl)-4H-benzo[1,4]thiazin-3-one 
• 137-07-5 2-amino-benzenethiol 

Relevant academic research and scientific papers

The discovery of N -[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy] ethoxy]-4-pyrimidinyl]- N ′-propylsulfamide (macitentan), an orally active, potent dual endothelin receptor antagonist

Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy. This led to the discovery of a novel series of alkyl sulfamide substituted pyrimidines. Among these, compound 17 (macitentan, ACT-064992) emerged as particularly interesting as it is a potent inhibitor of ETA with significant affinity for the ET B receptor and shows excellent pharmacokinetic properties and high in vivo efficacy in hypertensive Dahl salt-sensitive rats. Compound 17 successfully completed a long-term phase III clinical trial for pulmonary arterial hypertension.

beta -thiopropionyl-aminoacid derivatives and their use as beta -lactamase inhibitors

PCT No. PCT/EP97/00516 Sec. 371 Date Jan. 13, 1999 Sec. 102(e) Date Jan. 13, 1999 PCT Filed Feb. 3, 1997 PCT Pub. No. WO97/30027 PCT Pub. Date Aug. 21, 1997A method of treatment of bacterial infections in humans or animals which comprises administering, in combination with a beta -lactam antibiotic, a therapeutically effective amount of an amino acid derivative of Formula (I) or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R1 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms or by a mercapto, (C1-6)alkoxy, hydroxy, amino, nitro, carboxy, (C1-6)alkylcarbonyloxy, (C1-6)alkoxycarbonyl, formyl or (C1-6)alkylcarbonyl group, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl(C1-6)alkyl, heterocyclyl or heterocyclyl(C1-6)alkyl; R2 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C3-7)cycloalkyl, fused aryl(C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl-(CHR10)m-X-(CHR11)n, heterocyclyl or heterocyclyl-(CHR10)m-X-(CHR11)n, where m is 0 to 3, n is 1 to 3, each R10 and R11 is independently hydrogen or (C1-4)alkyl and X is O, S(O)x where x is 0-2, or a bond; R4 is hydrogen, or an in vivo hydrolysable acyl group; and R5 and R6 are independently hydrogen and (C1-6)alkyl or together represent (CH2)p where p is 2 to 5. Some compounds are claimed per se.

DEFLUORINATION REACTIONS OF gem-DIFLUORO- AND MONOFLUOROOLEFINS. NOVEL METHODS FOR ONE-CARBON HOMOLOGATIONS OF CARBONYL COMPOUNDS LEADING TO ALDEHYDES, CARBOXYLIC ACIDS, AND ESTERS

Defluorinative hydrolysis (or alcoholysis) of gem-difluoroolefins (1) easily prepared via the facile difluoromethylenation of carbonyl compounds afforded the carboxylic acids (or esters).The homologation method was applied to the synthesis of anti-inflammatory ibuprofen.Furthermore, defluorinative hydrolysis of monofluoroolefins obtained via the reduction of 1 gave the aldehydes.

Method of preparing arylacetic acid alkyl esters

In a process of producing an alkyl ester of a substituted or unsubstituted arylacetic acid wherein a substituted or unsubstituted aromatic halogen methyl compound is reacted with carbon monoxide and an alcohol having an alkoxy group the same as that of said ester, the improvement which comprises carrying out said reaction in a basic reaction medium in the presence as catalyst of: A. cobalt salt, metal or metal alloy and a sulfur compound, or B. a metal carbonyl compound.