749921-33-3

Upstream product

• 455-14-1 4-trifluoromethylphenylamine 
• 30414-53-0 methyl propanoyl acetate 
• 749921-32-2 methyl 3-(4-trifluoromethylphenylamino)-2-pentenoate 
• 1027896-34-9 (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone 
• 124-41-4 sodium methylate 
• 67-56-1 methanol 
• 192379-68-3 3-(trans-2'-pentenoyl)oxazolidin-2-one 

Downstream Products

• 667937-05-5 (3R)-3-(4-trifluoromethylphenylamino)pentanoic acid amide 

Relevant academic research and scientific papers

PROCESS FOR PRODUCING AMINO ACID DERIVATIVES

The present invention relates to a process for producing amino acid derivatives such as optically active β-amino acid in short steps with good yield and high optical purity, which comprises reacting a keto acid of the formula (1): wherein R1 is hydrogen, an optionally substituted hydrocarbon, etc.; R2 is a spacer; and R3 is an optionally substituted alkoxy, etc., or a salt thereof, with ammonia or an amine or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid and/or a fluorine-containing alcohol, to give an amino acid derivative of the formula (2): wherein Q is a group formed by removing one hydrogen atom from ammonia or an amine; X' is an acid and/or a fluorine-containing alcohol; and b is 0 or 1.

METHOD FOR PRODUCING AN OPTICALLY ACTIVE TETRAHYDROQUINOLINE

The present invention provides an industrially advantageous production method of optically active tetrahydroquinolines of formula (1), which comprises: 1) a step of reacting a β-ketoester of formula (2) with an amine of formula (3) to produce an enaminoester of formula (4); 2) a step of subjecting the enaminoester of formula (4) above obtained in 1) to asymmetric hydrogenation to produce an optically active β-amino acid derivative of formula (5); 3) a step of amidating the optically active β-amino acid derivative (5) above obtained in 2) to produce an amide of formula (6); 4) step of alkoxycarbonylating the amide of formula (6) above obtained in 3) to produce a compound of formula (7); and 5) a step of subjecting the compound of formula (7) above to cyclization to produce the optically active tetrahydroquinoline of formula (1).

Amine-salt-controlled, catalytic asymmetric conjugate addition of various amines and asymmetric protonation

Matrix presented. The combined use of chiral Pd complex 2 and amine salt enabled completely regulated release of free nucleophilic amine. Under these conditions, an efficient catalytic asymmetric conjugate addition of various amines was achieved to afford

Method for producing (R) -3- [4- (trifluoromethyl) phenylamino] -pentanoic acid amide derivative

The present invention provides a method for easily producing an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative useful for an intermediate for pharmaceutical products, particularly an inhibitor of a cholesteryl ester transfer protei