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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 32, Number 2
JKCSEZ 32(2)
April 20, 1988 

 
Title
New Synthetic Route to 1, 4-Dihydropyridine Monoacid Derivatives

1, 4-디히드로피리딘산 유도체의 새로운 제조방법에 관한 연구
Author
Young Key Shim, Sang Hee Lee, Jae Sung Kang, Wan Joo Kim

심영기, 이상희, 강재성, 김완규
Keywords
Abstract
의약적으로 매우 유용한 1,4-디하히드로피리딘 3,5-디카르복실산 에스테르의 중간체인 1,4-디히드로피리딘 모노 유기산(Ⅴ)을 알릴에스테르(Ⅳ)에 팔라듐 아세테이트 촉매를 사용하여 94%의 높은 수율로 얻었으며 이 중간체를 사용하여 2-(N-벤질-N-메틸아미노) 에틸메틸 2,6-디메틸-4-(3'-니트로페닐)-1,4-디히드로피리딘-3,5-디카르복실산 에스테르(Ⅶ) 및 그 유도체들을 70∼85%의 좋은 수율로 합성하였다.

A novel synthetic route to 1,4-dihydropyridine mono carboxylic acid derivatives is described. Allyl methyl 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate (Ⅳ) was treated with Pd(OAc)2 in dioxane for 30 min at 110℃ with reflux to give the mono acid compound(Ⅴ) in 94% yield. The mono acid intermediate was converted to 2-(N-benzyl-N-methylamino)ethyl methyl 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate (Ⅶ) (Nicardipine) and their derivatives in 70∼85% yield.

Page
144 - 148
Full Text
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