537-11-1Relevant academic research and scientific papers
N-SUBSTITUTED-CYCLIC AMINO DERIVATIVE
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Page/Page column 178, (2012/05/20)
The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is -N(R1b)-, G2 is -CO-, G3 is -C(R1c)(R1d)-, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c, and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
Formate ester synthesis via reaction of 2-bromoethylamines with dimethylformamide
Dakanali, Marianna,Tsikalas, George K.,Krautscheid, Harald,Katerinopoulos, Haralambos E.
, p. 1648 - 1651 (2008/09/19)
2-Bromoethylamines are converted to the corresponding formate esters in the presence of DMF. Both primary and secondary bromides are smoothly transformed to the esters in satisfactory yields. The reaction mechanism involves the formation of an aziridinium ion, which upon reaction with DMF forms a Vilsmeier-type intermediate that is further hydrolyzed to the corresponding formates. Participation of the β-amino group appears to control not only the regioselectivity but also the stereoselectivity of the reaction. Application of the reaction conditions to chiral substrates indicated that non-rearranged products are formed with retention of configuration at the reacting center.
Efficient synthesis of β-amino bromides
Nagle, Advait S.,Salvatore, Ralph N.,Chong, Byong-Don,Woon Jung, Kyung
, p. 3011 - 3014 (2007/10/03)
β-Aminoalcohols were smoothly converted to β-amino bromides using thionyl bromide and DMF, which were easily isolated without any further purification. Participation by the β-amino group in brominations not only enhanced reaction rates but also promoted stereo- and regioselectivities. (C) 2000 Elsevier Science Ltd.
