テネリグリプチン臭化水素酸塩水和物

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H413：長期的影響により水生生物に有害のおそれ

• 注意書き

  P273：環境への放出を避けること。

  P501：内容物/容器を．．．に廃棄すること。

テネリグリプチン臭化水素酸塩水和物 化学特性,用途語,生産方法

• 効能

  糖尿病治療薬, DPP-4阻害薬

• 商品名

  テネリア (田辺三菱製薬)

• 使用

  Teneligliptin Hydrobromide (2:5) is a dipeptidyl peptidase-4 (DPP-4) inhibitor that is used to treat type 2 diabetes. It is eliminated via excretion, and has a half-life of 24.2 hours in the human body.

• 臨床応用

  Teneligliptin is a DPP-4 inhibitor which was approved in Japan in 2012 for the treatment of type II diabetes. It was discovered and developed by Mitsubishi Tanabe Pharma under the trade name Tenelia®. Similar to other marketed DPP-4 inhibitors, teneligliptin was well tolerated in all studies and QD dosing produced a long-lasting inhibitory action against DPP-4 and an increase in active GLP-1 levels, with very low rates of renal excretion.

• 合成

  The only reported synthesis of teneligliptin is described in the scheme below. Reaction of commercially available N-Boc-piperazine (158) with diketene (159) in DMF at room temperature gave acetoacetamide 160 in 86% yield, and this material was immediately condensed with phenylhydrazine in methanesulfonic acid followed by a cyclodehydration with phosphorus oxychloride to give pyrazole 161 in 12% yield. The t-butyl carbamate was then removed with TFA in dichloromethane to give amine 162 in 88% yield. This amine was then subjected to butyrolactam 165 (which was prepared from N-Boctrans- 4-hydroxy-L-proline (163) coupled with thiazolidine (164) under conventional amide-forming conditions using EDC) in the presence of sodium triacetoxy borohydride (STAB-H) in acetic acid. This reductive amination reaction afforded the cis-aminopyrrolidine 166 exclusively in 50% yield. Removal of the t-butyl carbamate group with TFA afforded the teneligliptin free amine in 93% yield, and this freebase was then subsequently treated with 48% hydrobromic acid in refluxing ethanol to give teleligliptin hydrobromide hydrate (XXV) in 90% yield.

  

テネリグリプチン臭化水素酸塩水和物 生産企業

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テネリグリプチン臭化水素酸塩水和物 スペクトルデータ(MS)

906093-29-6, テネリグリプチン臭化水素酸塩水和物 キーワード