195194-80-0Relevant articles and documents
Iridium-catalyzed reductive nitro-mannich cyclization
Gregory, Alex W.,Chambers, Alan,Hawkins, Alison,Jakubec, Pavol,Dixon, Darren J.
, p. 111 - 114 (2015)
A new chemoselective reductive nitro-Mannich cyclization reaction sequence of nitroalkyl-tethered lactams has been developed. Relying on the rapid and chemoselective iridium(I)-catalyzed reduction of lactams to the corresponding enamine, subsequent nitro-
Iridium-Catalyzed Aza-Spirocyclization of Indole-Tethered Amides: An Interrupted Pictet-Spengler Reaction
Gabriel, Pablo,Gregory, Alex W.,Dixon, Darren J.
supporting information, p. 6658 - 6662 (2019/08/30)
A mild, reductive spirocyclization of indole-linked amides and lactams for the efficient and selective synthesis of aza-spirocyclic indoline products is described. The catalytic reductive activation of tertiary amides or lactams by Vaska's complex with tetramethyldisiloxane as the terminal reductant allowed iminium ion formation, before a diastereoselective 5-endo-trig spirocyclization of the tethered indole moiety was triggered. Terminal reduction affords the aza-spiroindoline products in an overall highly chemoselective and diastereoselective one-pot process.
5-memberd heteroaryl substituted 1,4-dihydropyridine compounds as bradykinin antagonists
-
, (2008/06/13)
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein A is independently halo; Y1 is —(CH2)m—, C(O) or S(O); Y2 is N or CH; R1 and R2 are independently C1-4 alkyl; R3 is selected from the following: (a) optionally substituted —(CH2)p—C3-7 cycloalkyl; (b) optionally substituted —C5-7 alkyl; and (c) substituted —C1-4 alkyl; and (d) optionally substituted C7- bicycloalkyl; R4 is optionally substituted thiazolyl, imidazolyl or oxazolyl; X is S, —NH, —N—C1-4 alkyl or O; R5 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl or halo; m is 0, 1 or 2; n is 0, 1, 2, 3, 4 or S; and p is 0, 1, 2, 3, 4, 5 or 6. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound.
