69 results about "Butylone" patented technology

The invention provides a process for preparing 3-hydroxy-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one (Formula I), into its racemic (R / S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms comprising: a) reacting 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-one of formula (III) with a suitable oxidoreductase enzymes or its suitable variants in the presence of suitable conditions and co-factor; and b) isolating 3-hydroxy-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one, into its racemic (R / S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms.

The present invention relates to a polypeptide having an activity to asymmetrically reduce (3S)-1-chloro-3-tert-butoxycarbonylamino-4-phenyl-2-butanone to produce (2R,3S)-1-chloro-3-tert-butoxycarbonylamino-4-phenyl-2-butanol isolated from a microorganism belonging to the genus Ogataea, a DNA encoding the polypeptide and a transformant that produces the polypeptide. The present invention moreover relates to a method of producing (2R,3S)-1-chloro-3-tert-butoxycarbonylamino-4-phenyl-2-butanol utilizing the polypeptide or the transformant. Using the polypeptide or transformant of the present invention, optically active alcohols such as (2R,3S)-1-chloro-3-tert-butoxycarbonylamino-4-phenyl-2-butanol and the like can be produced efficiently.

Hydroxy-substituted azetidinone hypocholesterolemic agents of the formulaor a pharmaceutically acceptable salt thereof, wherein:Ar1 and Ar2 are aryl or R4-substituted aryl;Ar3 is aryl or R5-substituted aryl;X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—;R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7;R1 and R3 are H or lower alkyl;q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5;R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CON6R7, —(lower alkylene)COOR6 and —CH═CH—COOR6;R6, R7 and R8 are H, lower alkyl or aryl-substituted IcR9 is lower alkyl, aryl or aryl-substituted lower alkyl;are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.

The present invention refers to highly functionalised spiro-fused azetidinones of formula I:having a cyclohexane moiety with the desired number of protected or unprotected hydroxyl groups which are introduced with high stereo and regioselectivity, as well as processes for their synthesis.

The invention discloses an environment-friendly plastic material. The material is prepared from, by weight, 50-120 parts of nylon, 42-78 parts of cis-hexenyl dicarboxylic anhydride-allyl benzene copolymer, 35-65 parts of 2-hydroxyl-4-octyl oxyl phenylbutyrophenone, 20-38 parts of butenyl distearamide, 15-30 parts of polybutylene terephthalate, 12-25 parts of polyether glycerol, 10-20 parts of brominated paraffin, 10-15 parts of olive oil, 8-14 parts of AR glass fiber, 6-12 parts of carboxyethyl cellulose, 15-25 parts of filler, 8-12 parts of addition agent, 4-6 parts of fire retardant, 3-5 parts of antismoke agent, 1-3 parts of ultraviolet light absorber, 1-3 parts of tackifier and 1-2 parts of softening agent. The environment-friendly plastic material is good in flame retardant effect, high in anti-impact capacity, high in toughness and good in performance, is low in preparation cost, can be applied and popularized and has remarkable economic and social benefits.

The invention discloses a synthesis method of a larotrectinib intermediate, and belongs to the field of drug synthesis. The method uses 4-chloro-1-(2, 5-difluorophenyl)butane-1-one (I) as the raw material to synthesize 5-(2, 5-difluorophenyl)-3, 4-dihydro-2H-pyrrole (III) through ammonolysis and ring closing one-pot method. The invention provides the synthesis method of the larotrectinib intermediate. The method is controllable in reaction process, easy to operate and high in yield.

The invention discloses an amine transaminase AcATA mutant and its application in the preparation of a sitagliptin intermediate. The amine transaminase AcATA mutant is obtained by performing a single mutation at position 122 of the amino acid sequence shown in SEQ ID No.2; Among them, the methionine at position 122 is mutated into histidine, valine or phenylalanine. The present invention obtains sites that may affect its catalytic activity through methods such as molecular docking and homologous modeling, and performs site-directed mutation. The finally obtained aminotransferase AcATA mutant not only has higher enzyme activity, but the enzyme activity is higher than 460U / g, which is more than 4 times that of the wild type; and can efficiently catalyze the sitagliptin intermediate precursor ketone 1-piperidine-4-(2,4,5-trifluorophenyl)-1,3-di Sitagliptin intermediate (R)-3-amino-1-piperidine-4-(2,4,5-trifluorophenyl)-1-butanone was synthesized from butanone, and the conversion rate was as high as 90% in 24 hours.