Carebastine Methyl Ester synthesis

4synthesis methods

Product Name:Carebastine Methyl Ester
CAS Number:189064-48-0
Molecular formula:C33H39NO4
Molecular Weight:513.6671

1-Butanone, 1-(4-bromophenyl)-4-[4-(diphenylmethoxy)-1-piperidinyl]-

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DIMETHYLKETENE METHYL TRIMETHYLSILYL ACETAL

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$38.00/5g

189064-48-0
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$95.00/1mg

Yield:189064-48-0 67.8%

Reaction Conditions:

with zinc(II) fluoride;tris-(dibenzylideneacetone)dipalladium⁽⁰⁾;tri-tert-butyl phosphine in DMF (N,N-dimethyl-formamide) at 80; for 2 h;Product distribution / selectivity;

Steps:

8

EXAMPLE 8; One and seven-tenths grams of 3, 90 mg of P(tBu)₃, 300 mg of Pd(dba)₂, 250 mg of ZnF₂and 1.1 g of 5 were dissolved in 330 mL of DMF under argon. The mixture was heated to 80° for two hours, cooled to room temperature, diluted with ether and worked up as described in example 1. The resulting product was filtered through silica to provide 1.2 g (67.8%) of 6.

References:

US2006/63933,2006,A1 Location in patent:Page/Page column 11-12; 14; 16; 21