169750-73-6

Usage

Uses

Used in Pharmaceutical Industry:
C-(4-BENZYL-MORPHOLIN-3-YL)-METHYLAMINE is used as a building block in the development of new drugs for its potential pharmacological activities. The presence of a morpholine ring in its structure may contribute to its therapeutic effects, making it a promising candidate for the creation of novel pharmaceutical agents.
Used in Organic Synthesis:
C-(4-BENZYL-MORPHOLIN-3-YL)-METHYLAMINE is used as a key intermediate in organic synthesis for the production of various chemical compounds. Its unique structure allows for further functionalization and modification, enabling the synthesis of a wide range of organic molecules with diverse applications.
Used in Research and Development:
C-(4-BENZYL-MORPHOLIN-3-YL)-METHYLAMINE is utilized in research and development for understanding its properties, reactivity, and potential applications. Its synthesis and characterization provide valuable insights into the behavior of amines with complex structures, contributing to the advancement of chemical knowledge and innovation in the pharmaceutical and chemical industries.

Upstream product

• 170701-84-5 N-(4-benzylmorpholin-3-yl)methylacetamide 
• 106973-37-9 (3S)-5-oxo-4-(phenylmethyl)-3-morpholinecarboxylic acid 

Relevant academic research and scientific papers

Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors

Described herein are the discovery and structure-activity relationship (SAR) studies of the third-generation 4-H heteroaryldihydropyrimidines (4-H HAPs) featuring the introduction of a C6 carboxyl group as novel HBV capsid inhibitors. This new series of 4-H HAPs showed improved anti-HBV activity and better drug-like properties compared to the first- and second-generation 4-H HAPs. X-ray crystallographic study of analogue 12 (HAP_R01) with Cp149 Y132A mutant hexamer clearly elucidated the role of C6 carboxyl group played for the increased binding affinity, which formed strong hydrogen bonding interactions with capsid protein and coordinated waters. The representative analogue 10 (HAP_R10) was extensively characterized in vitro (ADMET) and in vivo (mouse PK and PD) and subsequently selected for further development as oral anti-HBV infection agent.

Synthesis and structure-activity relationships of 4-amino-5-chloro-2- ethoxybenzamides with six- and seven-membered heteroalicycles as potential gastroprokinetic agents

A new series of 4-amino-5-chloro-2-ethoxybenzamides 3b-f and 5-8 bearing six- and seven-membered heteroalicycles was prepared and evaluated for gastroprokinetic activity. Compounds 3b-e, derived by replacement of the morpholine oxygen of 4-amino-N-[(4-benzyl-2-morpholinyl)methyl]-5-chloro-2- ethoxybenzamide (3a) with other atoms (sulfur, nitrogen and carbon), generally exhibited a potent gastric emptying activity. N-(4-Benzyl-3- morpholinyl)methylbenzamide (5a) and its analogues 5b-e had weaker activity. However, N-(4-benzyl-3-morpholinyl)ethylbenzamide 8 was as potent as 3a. Benzamides 6a-e, having seven-membered heteroalicycles, showed fairly potent activity. Molecular superimpositions of 5a, 6a and 8 upon 3a using computer graphics suggested that the direction of the N-benzyl group greatly influences the gastric emptying activity, whereas the location of the alicyclic nitrogen is less critical.