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ChemicalBook CAS DataBase List Cetirizine Descarboxymethyl R-Isomer
705289-61-8

Cetirizine Descarboxymethyl R-Isomer synthesis

2synthesis methods
109806-71-5 Synthesis
4-[(4-CHLOROPHENYL)PHENYLMETHYL]-1-PIPERAZINEETHANOL DIHYDROCHLORIDE

109806-71-5
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Cetirizine Descarboxymethyl R-Isomer

705289-61-8
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Yield:99 % ee

Reaction Conditions:

at 25;Resolution of racemate;

Steps:

1.1.3 1.3 Preparation of compound 1b (compound of formula I in free form wherein n=2. Y=OH, (R)-enantiomer):

The chromatographic separation of the enantiomers of compound la such as obtained in 1.2 is performed using 8 columns of 4.8 x 11.3 cm for 1 kg of chiral stationary phase CHIRALPAK AD (DAICEL) with methanol as the eluent. The chromatographic parameters are: K'1 (capacity factor of the R-enantiomer) = 0. 525 k'2 (capacity factor of the S-enantiomer) = 1. 111 Alpha (selectivity factor) = 2. 118 Resolution = 2. 164 Temperature = 23°C PURITY OF (R) -ENANTIOMER IS 99.5 %; EE = 99 %

References:

WO2004/65360,2004,A2 Location in patent:Page 9

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