(1R,9R,10R)-4-(trideuteriomethoxy)-17-(trideuteriomethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-triene

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: (1R,9R,10R)-4-(trideuteriomethoxy)-17-(trideuteriomethyl)-17-azatetracyclo[7.5.3.01,10.02,7]heptadeca-2(7),3,5-triene
• 化学式: C18H25NO
• 分子量: 277.4
• InChiKey: MKXZASYAUGDDCJ-IBPZTRMUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] INDUSTRIAL PROCESS OF MONO-ALKYLATING A PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVES WITH DEUTERATED-ALKYL<br/>[FR] PROCÉDÉ INDUSTRIEL DE MONOALKYLATION D'UN AZOTE DE PIPÉRIDINE DANS DES DÉRIVÉS DE LA PIPÉRIDINE AVEC UN ALKYLE DEUTÉRÉ
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2019049918A1

  公开（公告）日：2019-03-14

  The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.

  本发明涉及一种用氘代低烷基对哌啶衍生物中的哌啶氮进行单烷基化的方法，包括用芳基保护基保护哌啶氮，使用氘代低烷基化试剂在中性或碱性条件下对哌啶氮进行低烷基化，然后去除芳基保护基。
• Industrial process of mono-alkylating piperidine nitrogen in piperidine derivative with deuterated-lower-alkyl
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：US11214545B2

  公开（公告）日：2022-01-04

  The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.

  本发明涉及一种用氚化低烷基对哌啶衍生物中的哌啶氮进行单烷基化的方法，该方法包括用芳烷基保护基团保护哌啶氮，在中性或碱性条件下用氚化低烷基化剂对哌啶氮进行低烷基化，然后对芳烷基保护基团进行脱保护。
• INDUSTRIAL PROCESS OF MONO-ALKYLATING A PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVES WITH DEUTERATED-ALKYL
  申请人：Otsuka Pharmaceutical Co., Ltd.

  公开号：EP3679018A1

  公开（公告）日：2020-07-15
• INDUSTRIAL PROCESS OF MONO-ALKYLATING PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVE WITH DEUTERATED-LOWER-ALKYL
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：US20200407326A1

  公开（公告）日：2020-12-31

  The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.