116290-77-8Relevant academic research and scientific papers
Concise Synthesis of Vesnarinone and Its Analogues by Using Pd-Catalyzed C-N Bond-Forming Reactions
See, Yi Yang,Dang, Tuan Thanh,Chen, Anqi,Seayad, Abdul Majeed
, p. 7405 - 7412 (2014)
An efficient and concise synthesis of vesnarinone and its analogues from readily available starting materials and by using catalytic C-N bond-forming reactions is reported. In this protocol, a homogeneous Pd-catalyzed Buchwald-Hartwig amination and a supported Pd nanoparticles catalyzed aminocarbonylation were utilized as the two key reactions to prepare vesnarinone in an overall yield of 73 %. Sixteen analogues were also synthesized in up to 89 % overall yield. An efficient and concise synthesis of vesnarinone was achieved in three steps by using palladium-catalyzed C-N bond-forming reactions, which included the Buchwald-Hartwig amination and an aminocarbonylation reaction. High overall yields were obtained by using this strategy for the preparation of several vesnarinone analogues.
Pyrrolopyrimidine A2b selective antagonist compounds, their synthesis and use
-
Page 32, (2010/02/06)
The subject invention provides compounds having the structure: 1 wherein,R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O)Ra;R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O)Ra, orR1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(═O)OH;R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb;R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl;R5 is —(CH2)mOR6, —CHNOR7, —C(═O)NR8R9, —(CH2)mC(═O)OR10, —(CH2)kC(═O)NR11R12;wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring;R7 is hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl;R8 and R9 are each independently hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl, (C1-C30)alkylamino, (C1-C30)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, orR8, N, and R9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring;R10 is hydrogen or a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring;R11, N and R12 together form a 4-8 membered heterocyclic ring;Ra and Rb are each independently hydrogen or alkyl;m is 0, 1, 2 or 3; andk is 1, 2 or 3,or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.
