Novel N-(4-piperidinyl)-N-phenylamides and -carbamates having very potent analgesic activity, methods of preparing same and useful intermediates therefor.
新型具有非常强的镇痛活性的N-(4-哌啶基)-N-苯基酰胺和-碳酸酯,其制备方法及有用的中间体。
SUBSTITUTED 4-AMINO-PIPERIDINES
申请人:Gant Thomas G.
公开号:US20100016365A1
公开(公告)日:2010-01-21
The present invention relates to new substituted 4-amino-piperidine opioid receptor modulators, pharmaceutical compositions thereof, and methods of use thereof.
本发明涉及新的取代4-氨基哌啶类阿片受体调节剂,其药物组成物以及使用方法。
N-(4-piperidinyl)-N-phenylamides and -carbamates
申请人:Janssen Pharmaceutica N.V.
公开号:US03998834A1
公开(公告)日:1976-12-21
Novel N-(4-piperidinyl)-N-phenylamides and -carbamates having very potent analgesic activity, methods of preparing same and useful intermediates therefor.
THE NEW PROCESS FOR PRODUCING N-PHENYL-N-(4-PIPERIDINYL) AMIDE DERIVATIVES SUCH AS REMIFENTANIL AND CARFENTANIL
申请人:Bioka s. r.o.
公开号:EP3199523A1
公开(公告)日:2017-08-02
Disclosed is a process for the preparation of the compound of formula (I):
which comprises reacting a compound of formula (II):
with acylating agent of formula (IV) in the presence of orthoester of formula (III) in an aprotic solvent:
The process may be used for synthesizing derivatives of fentanyl. Specifically set out are pathways for synthesizing remifentanil and carfentanil. The disclosed process require fewer steps and produce a greater yield of products than methods reported in the prior art.
A compound having a partial structure represented by the formula (A)
(wherein ring Xa represents a nitrogen-containing ring and R represents optionally substituted amino) or a salt thereof. The compound or salt is highly effective in regulating neuromedin U receptors and is useful as a preventive/therapeutic agent for hypertension, etc.