1062136-14-4Relevant academic research and scientific papers
Compound I and (R)- 3 - amino piperidine hydrochloride II, its preparation method and its application in the synthesis of advantage geleg sandbank
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Paragraph 0137; 0139-0143; 0146-0147; 0150-155, (2017/10/22)
The invention discloses a preparation method of 3-aminopiperidine and its derivative with optical activity and an application of the compound and its derivative in synthesis of a dipeptidyl peptidase-IV inhibitor Linagliptin. According to the preparation
Enantioselective synthesis and physicochemical properties of libraries of 3-amino- and 3-amidofluoropiperidines
Orliac, Aurelie,Routier, Julie,Burgat Charvillon, Fabienne,Sauer, Wolfgang H. B.,Bombrun, Agnes,Kulkarni, Santosh S.,Gomez Pardo, Domingo,Cossy, Janine
supporting information, p. 3813 - 3824 (2014/04/03)
The enantioselective syntheses of 3-amino-5-fluoropiperidines and 3-amino-5,5-difluoropiperidines were developed using the ring enlargement of prolinols to access libraries of 3-amino- and 3-amidofluoropiperidines. The study of the physicochemical properties revealed that fluorine atom(s) decrease(s) the pKa and modulate(s) the lipophilicity of 3-aminopiperidines. The relative stereochemistry of the fluorine atoms with the amino groups at C3 on the piperidine core has a small effect on the pK a due to conformationnal modifications induced by fluorine atom(s). In the protonated forms, the C-F bond is in an axial position due to a dipole-dipole interaction between the N-H+ and C-F bonds. Predictions of the physicochemical properties using common software appeared to be limited to determine correct values of pKa and/or differences of pK a between cis- and trans-3-amino-5-fluoropiperidines.
AMIDOBIPIPERIDINECARBOXYLATE M1 ALLOSTERIC AGONISTS, ANALOGS AND DERIVATIVES THEREOF, AND METHODS OF MAKING AND USING SAME
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Page/Page column 80, (2010/09/17)
In one aspect, the invention relates to compounds having a general structure: Formula (I) which are useful as allosteric agonists of the M1 muscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
