81102-38-7Relevant articles and documents
Glucosamine modified pentacyclic piperazine diketone and preparation and application thereof (by machine translation)
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Paragraph 0023; 0029-0030, (2020/12/14)
Aminoglucose-modified pentacyclic piperazinedione, and preparation and application thereofCH in the following formula is disclosed. 2 CO- Aminoglucose-modified pentacyclic piperazinedione The invention discloses a synthetic method thereof, disc
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.
BICYCLIC PYRAZOLE DERIVATIVE
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Page/Page column 179, (2010/11/30)
A compound represented by the following formula (I), a prodrug thereof, or a pharmaceutically acceptable salt of either. These are compounds having high DPP-IV inhibitory activity and improved in safety, nontoxicity, etc. (I) [In the formula, R1 represents hydrogen, optionally substituted alkyl, etc.; the solid line and dotted line between A1 and A2 indicate a double bond (A1=A2), etc.; A1 represents a group represented by the formula C(R2), etc.; A2 represents a group represented by the formula C(R4), etc.; R2 represents hydrogen, optionally substituted alkyl, etc.; R4 represents hydrogen, optionally substituted alkyl, etc.; R6 represents hydrogen, optionally substituted aryl, etc.; and -Y represents, e.g.; a group represented by the formula (A): (A) (wherein ml is 0, 1, 2, or 3; and R7 is absent, or one or two R7's are present and each independently represents optionally substituted alkyl, etc.).]