摘要:
A process for the in situ preparation of chiral compounds derived from oxazaborolidine-borane complexes, wherein a metal borohydride, a Lewis base and an inorganic acid ester are brought together and an optically active amino alcohol and optionally a halide are then added. The compound obtained is a complex that is useful as a catalyst in asymmetric reduction reactions. The reaction is performed by adding the substance to be reduced, particularly prochiral ketones or ether oximes, in order to synthesize chiral alcohols or chiral amines.
摘要:
A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, which comprise: a hydrogenation/isomerization reaction in presence of a heterogeneous catalyst, of an oxime derivatives of formula (II) where R1, R2 and R3 are as defined above with an acyl derivative of formula (III) (R4CO)mX wherein R4, m and X are as defined above.
摘要:
A process for the in situ preparation of chiral compounds derived from oxazaborolidine-borane complexes, wherein a metal borohydride, a Lewis base and an inorganic acid ester are brought together and an optically active amino alcohol and optionally a halide are then added. The compound obtained is a complex that is useful as a catalyst in asymmetric reduction reactions. The reaction is performed by adding the substance to be reduced, particularly prochiral ketones or ether oximes, in order to synthesize chiral alcohols or chiral amines.
摘要:
A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, which comprise: a hydrogenation/isomerization reaction in presence of a heterogeneous catalyst, of an oxime derivatives of formula (II) wherein R1, R2 and R3 are as defined above with an acyl derivative of formula (III) (R4CO)mX wherein R4, m and X are as defined above.
摘要:
A process for the preparation of optically active substituted alpha-amino-indane derivatives of formula (I), which include: an asymmetric hydrogenation reaction of an en-amide derivative of formula (III) in presence of hydrogen and an optically active catalyst, in order to obtain an amide derivative of formula (II), a hydrolysis reaction of the amide derivative of formula (II) obtained in the previous step,in order to obtain optically active substituted alpha-amino-indane derivatives of formula (I).
摘要:
A process is for the preparation of optically active substituted alpha-indanyl amide derivatives of formula (I), which include: an asymmetric hydrogenation reaction of an en-amide derivative of formula (III) in presence of hydrogen and an optically active catalyst, in order to obtain an amide derivative of formula (II), a hydrolysis reaction of the amide derivative of formula (II) obtained in the previous step, in order to obtain optically active-substituted alpha-indanyl amide derivatives of formula (I).
摘要:
A process is used for the preparation of 1,3,2-oxazaborolidine compounds.This process prepares compounds of formula (I) or (IA): in which: R1 is an alkyl or an aryl; and R2, R3, R4 and R5 are especially a hydrogen atom or an alkyl, wherein the following are reacted in two steps: a) a boric precursor compound with an acetal compound to give a boronate compound; and b) the boronate compound with an amino alcohol compound. This process avoids by-products and exhibits a very good stereospecificity.
摘要:
The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof.This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: wherein R independently represents hydrogen or a linear or branched C1-15 alkyl group.With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.
摘要:
An in situ or one-pot process for the preparation of the compounds of formula (I) uses a compound of general formula (I): and includes:a) the hydrogenation of a nitrile group of the compound of general formula (II): in which R1 to R4 are especially H or alkyl and n varies from 0 to 4, in the presence of a hydrogenation catalyst, a methylating agent and an organic acid as solvent, and at a temperature Ta below the initiation temperature of a reductive amination reaction, to give a primary amine from the nitrile group; andb) the reductive amination of the primary amine in the presence of hydrogen, at a temperature Tb above Ta, to give the dimethylated amine of general formula (I) by activation of the methylating age.
摘要:
The invention relates to a process for the preparation of substituted 2-vinyl-2-arylmorpholine derivatives as described herein. This invention also relates to 2-vinyl-2-arylmorpholine derivatives as well as intermediates therefor.