In the presence of trifluoroacetic anhydride, 5-bromo-2-chlorobenzoic acid and phenetole are selected to complete a direct acylation reaction under the catalysis of boron trifluoride diethyl etherate, and triethylsilane is added thereinto without treatment for one-pot reaction to obtain a target ...
The invention discloses a preparation method of empagliflozin. The preparation method comprises the steps of firstly, reacting 5-bromo-2-chlorobenzoic acid and anisole to obtain 5-bromo-2-chlorphenyl-4-methoxyphenyl-ketone V; carrying out reduction reaction on 5-bromo-2-chlorphenyl-4-methoxyphenyl-...
1. A process for the preparation of dapagliflozin in amorphous form, the process comprising: (a) reducing a compound of formula II to a compound of formula III in the presence of a Lewis acid; wherein the compound of formula II is prepared by reacting 5-bromo-2-chlorobenzoyl chloride with...
2. The process of claim 1 wherein: the reaction of (trans)-3-methylene-1,2-cyclopropanedicarboxylic acid and (R)-(+)-α-methylbenzylamine in step (a) is performed in the presence of isopropanol and water at an elevated temperature. ...
The following preparations of intermediates are also described: 2-Formyl-5-chlorobenzoic acid is reacted with PhMgBr forming 3 - phenyl - 6 - chlorophthalide (a); (a) is reduced with Zn in NH 3 to 2- benzyl - 5 - chlorobenzoic acid (b); (b) is converted to methyl 2-benzyl-5-...
5-dichloro-6-nitrobenzoic acid, 2,6-dimethoxy-3,5-dichlorobenzoic acid, 2-methoxy-3-chloro acid -5-methylphenylacetic acid, 2-methoxy-3,5-dichloro-6-bromobenzoic acid and 2-methoxy-3-chloro-6-methylbenzoic acid, said compound being in the form of the free acid, the anhydride, an amide...
a -naphthylacetic acid, b -naphthylacetic acid, b -naphthoxyacetic acid, b -naphthoxypropionic acid, anthracene-acetic acid, 2,3,6-trichlorobenzoic acid, 2,3,5- triiodo-benzoic acid, phenacetyl-leucine, maleic hydrazide, and esters, amides, inorganic salts and amine salts of any of the fo...
Acids include hydrogen chloride, hydrogen bromide, 100% sulphuric acid, chloroacetic acid, bromoacetic acid, cyanoacetic acid, dichloroacetic acid, trichloroacetic acid, o-chlorobenzoic acid, o-bromobenzoic acid, o-nitrobenzoic acid, 3,5-dinitrobenzoic acid. The reaction may be carried out in an ...
to give 2- (2-methyl-5-chlorophenylmercapto) - 4 - chlorobenzoic acid; (2) the method of (1) is used to prepare-2-(2-methyl-5-chlorophenyl-mercapto)-4-methyl - benzoic acid, and (3) the method of (1) is used to prepare 2-(2-methyl-5-chlorophenylmercapto)-4-methoxybenzoic acid...
This product may be hydrolysed by sulphuric acid to give chloromethyl-2, 3, 4-trichlorobenzoic acid. Example 2 relates to the preparation of di(chloromethyl) hexachlorotoluene starting from hexachlorocyclopentadiene and 1,4-dichloro-2-butyne. Example 3 relates to the preparation of phenyl-a , a...