64586-21-6Relevant articles and documents
Manganese-Catalyzed Oxidative Azidation of C(sp3)-H Bonds under Electrophotocatalytic Conditions
Niu, Linbin,Jiang, Chongyu,Liang, Yuwei,Liu, Dingdong,Bu, Faxiang,Shi, Renyi,Chen, Hong,Chowdhury, Abhishek Dutta,Lei, Aiwen
, p. 17693 - 17702 (2020)
The selective installation of azide groups into C(sp3)-H bonds is a priority research topic in organic synthesis, particularly in pharmaceutical discovery and late-stage diversification. Herein, we demonstrate a generalized manganese-catalyzed oxidative azidation methodology of C(sp3)-H bonds using nucleophilic NaN3 as an azide source under electrophotocatalytic conditions. This approach allows us to perform the reaction without the necessity of adding an excess of the substrate and successfully avoiding the use of stoichiometric chemical oxidants such as iodine(III) reagent or NFSI. A series of tertiary and secondary benzylic C(sp3)-H, aliphatic C(sp3)-H, and drug-molecule-based C(sp3)-H bonds in substrates are well tolerated under our protocol. The simultaneous gram-scale synthesis and the ease of transformation of azide to amine collectively advocate for the potential application in the preparative synthesis. Good reactivity of the tertiary benzylic C(sp3)-H bond and selectivity of the tertiary aliphatic C(sp3)-H bond in substrates to incorporate nitrogen-based functionality at the tertiary alkyl group also provide opportunities to manipulate numerous potential medicinal candidates. We anticipate our synthetic protocol, consisting of metal catalysis, electrochemistry, and photochemistry, would provide a new sustainable option to execute challenging organic synthetic transformations.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 73, (2010/08/09)
The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 43, (2008/06/13)
The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and method
4,1-benzoxazepines, their analogues, and their use as somatostatin agonists
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, (2008/06/13)
The present invention provides a compound of the formula: wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; Z is an optionally substituted cyclic group or linear hydrocarbon group; R1is a hydrogen atom, an optionally substituted hydrocarbon group or heterocyclic ring; R2is an optionally substituted amino group; D is a bond or an optionally substituted divalent hydrocarbon group; E is a bond, —CON(Ra)—, —N(Ra)CO—, —N(Rb)CON(Rc)—, —N(Rd)COO—, —N(Re)SO2—, —COO—, —N(Rf)—, —O—, —S— —SO—, —SO2—, (in which Ra, Rb, Rc, Rd, Reand Rfare respectively a hydrogen atom or an optionally substituted hydrocarbon group); G is a bond or an optionally divalent substituted hydrocarbon group; L is a divalent group; ring B may form an optionally substituted non-aromatic condensed nitrogen-containing heterocyclic ring by combining with R2; X is two hydrogen atoms, an oxygen atom or a sulfur atom;is a single bond or a double bond, and Y is a nitrogen atom whenis a double bond, or an oxygen atom, —N(R4)— (in which R4is a hydrogen atom, an optionally substituted hydrocarbon group or an acyl group) or S(O)n(in which n is 0, 1 or 2) whenis a single bond, or a salt thereof, which have somatostatin receptor agonistic action.
