29264-40-2Relevant articles and documents
A Mild and Convenient Procedure for Conversion of Alkenes into Alkyl Iodides via Reaction of Iodine Monochloride with Organoboranes
Kabalka, George W.,Gooch, Eugene E.
, p. 3578 - 3580 (1980)
Alkenes are rapidly converted to alkyl iodides under mild conditions via a hydroboration-iodination sequence which utilizes iodine monochloride as the iodination agent.The iodination proceeds with inversion of configuration.A series of functionally substituted iodides was synthesized via the new products.
Regiodivergent Conversion of Alkenes to Branched or Linear Alkylpyridines
Kim, Minseok,Shin, Sanghoon,Koo, Yejin,Jung, Sungwoo,Hong, Sungwoo
supporting information, p. 708 - 713 (2022/01/20)
Herein we report a practical protocol for the visible-light-induced regiodivergent radical hydropyridylation of unactivated alkenes using pyridinium salts. This approach provides a unified synthetic platform to control the regioselectivity of the synthesis of linear or branched C4-alkylated pyridines. A remarkable selectivity switch from the anti-Markovnikov to the Markovnikov product can be achieved by the addition of tetrabutylammonium bromide. The versatility of this protocol is further demonstrated based on the late-stage functionalization in pharmaceuticals.
Tautomycetin Synthetic Analogues: Selective Inhibitors of Protein Phosphatase I
Woydziak, Zachary R.,Yucel, A. John,Chamberlin, A. Richard
, p. 839 - 850 (2020/12/15)
Ser/Thr protein phosphatases (PPs) regulate a substantial range of cellular processes with protein phosphatases 1 (PP1) and 2 A (PP2A) accounting for over 90 % of the activity within cells. Nevertheless, tools to study PPs are limited as PPs inhibitors, particularly those selective for PP1 inhibition, are relatively scarce. Two examples of PP1-selective inhibitors, which share structural similarities, are tautomycin (TTM) and tautomycetin (TTN). This work describes the development of PP1/PP2A inhibitors that incorporate key structural features of TTM and TTN and are designed to conserve regions known to bind the active site of PP1/PP2A but vary regions that differentially contact the hydrophobic groove of PP1/PP2A. In all 28 TTN analogues were synthetically generated that inhibit PP1/PP2A activity at 50 values were determined for the seven most active analogues, which ranged from 34 to 1500 nM (PP1) and 70 to 6800 nM (PP2A). Four of the seven analogues possessed PP1 selectivity, and one demonstrated eightfold selectivity in the nanomolar range (PP1 IC50=34 nM, PP2A IC50=270 nM). A rationale is given for the observed differences in selectivity.
3,6-DIAMINO-PYRIDAZIN-3-YL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USES AS PRO-APOPTOTIC AGENTS
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Page/Page column 49, (2021/02/05)
Compounds of formula (I) wherein Het1, Het2, R1, R2 and R3 are as defined in the description. Medicaments.
