Welcome to chemicalbook!
Chinese English Japanese Germany Korea
400-158-6606
Try our best to find the right business for you.
Do not miss inquiry messages Please log in to view all inquiry messages.

Welcome back!

ChemicalBook CAS DataBase List Fexofenadine

Fexofenadine synthesis

8synthesis methods
-

Yield:83799-24-0 87%

Reaction Conditions:

Stage #1:4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid with potassium hydroxide in methanol at 0 - 20; for 1 h;
Stage #2: with potassium borohydride in methanol at 50; for 3 h;Reagent/catalyst;

Steps:

1.6
(6) 40 g (0.08 mol) of 4-{4-[4-(hydroxybenzhydryl)-1-piperidinyl]-1-butyryl group was placed in a 500 ml three-necked flask equipped with a magnetic stirrer. }-α,α-dimethyl-phenylacetic acid (VI) and 150 ml of methanol,After cooling to 0 ° C, 80 ml of 1 N potassium hydroxide solution was added dropwise, and after the dropwise addition was completed,After adding 4.32 g (0.08 mol) of potassium borohydride and returning to room temperature for 1 hour, an additional 2.16 g of potassium borohydride was added, and the mixture was heated to 50 ° C for 3 hours.The pH was then adjusted to 5 with 50% phosphoric acid to precipitate a solid which was filtered and washed with water.The wet product is recrystallized and purified by using methanol and water mixed solvent to obtain 35 g of high-purity fexofenadine (I), the yield is 87%, and the HPLC content is >99.7%;

References:

Chizhou Dongsheng Pharmaceutical Co., Ltd.;Huang Xiao;Bu Gonggaofamingren CN104557671, 2018, B Location in patent:Paragraph 0047; 0053; 0064; 0065

FullText

Fexofenadine Related Search: