METHOD FOR MAKING EP4 ANTAGONIST

To provide method for the synthesis of an EP4 antagonist that is suitable for mass production and is high in efficiency and cost-effectiveness.SOLUTION: The present disclosure provides methods for making compounds (I), including the step of reacting (1'S,2'R)-6-[(propane-2-yl)carbamoyl]-2,...

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Main Authors SARAH EVELYN STEINHARDT, CARLOS A GUERRERO, STEVEN R WISNIEWSKI, GREGORY LOUIS BEUTNER, PATRICIA Y CHO, MICHAEL BRYAN HAY, SAGAWA NAOYA, GUO XUELEI, JOHN RYAN COOMBS, ARIHARA RYOICHI, YU MIAO
Format Patent
LanguageEnglish
Japanese
Published 22.02.2023
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:To provide method for the synthesis of an EP4 antagonist that is suitable for mass production and is high in efficiency and cost-effectiveness.SOLUTION: The present disclosure provides methods for making compounds (I), including the step of reacting (1'S,2'R)-6-[(propane-2-yl)carbamoyl]-2,3-dihydrospiro[[1]benzopyran-4,1'-cyclopropane]-2'-carboxylic acid with a corresponding aniline derivative. The present disclosure also relates to intermediates useful in the methods.SELECTED DRAWING: None 【課題】大量生産に適した、効率的かつ費用対効果の高い、ＥＰ４アンタゴニストの合成法を提供する。【解決手段】（１'Ｓ，２'Ｒ）－６－［（プロパン－２－イル）カルバモイル］－２，３－ジヒドロスピロ［［１］ベンゾピラン－４，１'－シクロプロパン］－２'－カルボン酸と、対応するアニリン誘導体とを反応させる工程を含む、化合物（Ｉ）の製造方法である。本開示はまた、上記方法において有用な中間体に関する。TIFF2023025693000039.tif50170【選択図】なし
Bibliography:Application Number: JP20220126736