5-bromo-2-chloro-4’-ethoxydiphenylmethane literature
Synthesis method for preparing 5-bromo-2-chloro-4'-ethoxydiphenylmethane
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, (2022/04/08)
The present invention relates to a method for preparing 5-bromo-2-chloro-4'-ethoxydiphenylmethane, first of all o-chlorobenzoic acid chlorination made of o-chlorobenzoyl chloride, and then fuucylation to make 2-chloro-4'-iodobenzophenone, further brominated to make 5-bromo-2-chloro-4'-iododibenzophenone, and then reduced to make 5-bromo-2-chloro-4'-iododiphenylmethane, and finally by substitution reaction to make 5-bromo-2-chloro-4'-ethoxydiphenylmethane. The method of the present invention is streamlined, the resulting product purity is high, the raw materials used, excipients are common compounds, the use of low toxicity solvents and can be recycled, will not produce phosphorus-containing wastewater, high safety and environmental friendliness, low cost, low requirements for equipment, suitable for industrial production.
PREPARATION OF HIGHLY PURE AMORPHOUS DAPAGLIFLOZIN
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Page/Page column 24, (2021/12/13)
A novel and improved process for the preparation of amorphous dapagliflozin is disclosed. The present invention further provides pharmaceutical compositions containing amorphous dapagliflozin, optionally in a combination with one or more other active substances and methods for making the same.
Synthesis method of dapagliflozin intermediate 5-bromo-2-chloro-4 '-ethoxydiphenylmethane
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, (2020/04/06)
The invention discloses a synthesis method of a dapagliflozin intermediate 5-bromo-2-chloro-4 '-ethoxydiphenylmethane. The method comprises the following steps: using 5-bromo-2-chlorobenzoic acid as araw material to be acylated by thionyl chloride, and then carrying out acylation reaction with 1-nitro-4-(phenoxymethyl) benzene, reducing, acetylating, hydrogenating and ethylating to obtain the dapagliflozin intermediate 5-bromo-2-chloro-4'-ethoxydiphenylmethane. The method can effectively avoid the acylation reaction ortho-position by-product so that the preparation of dapagliflozin is convenient for quality control, the reaction is mild, the yield is high and the method has an industrial application prospect.
Preparation method of 5-bromo-2-chloro-4 '-ethoxydiphenylmethane
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Paragraph 0034; 0038; 0044-0060, (2020/09/23)
The invention relates to a preparation method of 5-bromo-2-chloro-4 '-ethoxydiphenylmethane. The preparation method is characterized by comprising the following steps: step S1, preparation of 5-bromo-2-chlorobenzoyl chloride, step S2, preparation of 5-bromo-2-chloro-4'-ethoxybenzophenone, and step S3, preparation of 5-bromo-2-chloro-4 '-ethoxydiphenylmethane. The invention further discloses the 5-bromine-2-chloro-4 '-ethoxydiphenylmethane prepared according to the preparation method of the 5-bromine-2-chloro-4'-ethoxydiphenylmethane. The invention further discloses the 5-bromine-2-chloro-4 '-ethoxydiphenylmethane prepared according to the preparation method of the 5-bromine-2-chloro-4'-ethoxydiphenylmethane. According to the preparation method of the 5-bromo-2-chloro-4 '-ethoxydiphenylmethane, traditional preparation process conditions are optimized and innovated, the method effectively improves the product purity, the reaction conversion rate and the production efficiency, has no special requirements on reaction conditions and equipment, is suitable for industrial production, causes less pollution to the environment and effectively realizes good combination of economic benefits, social benefits and ecological benefits.