- PURINONES AS UBIQUITIN-SPECIFIC PROTEASE 1 INHIBITORS
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The application relates to inhibitors of USP1 useful in the treatment of cancers, and other USP1 associated diseases and disorders, having the Formula: (I), where R1, R2, R3, R3', R4, R5, X1, X2, X3, X4, and n are described herein.
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Paragraph 00394
(2017/06/12)
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- Ionic liquid iodinating reagent for mild and efficient iodination of aromatic and heteroaromatic amines and terminal alkynes
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Hexamethylene bis(N-methylimidazolium) bis(dichloroiodate) (HMBMIBDCI), an ionic liquid iodinating reagent, have been prepared and characterized. Its ability to perform iodination reactions with a variety of substrates has been explored. In general, iodination reactions of aromatic and heteroaromatic amines proceed with good yields in the absence of solvent. Reactions of terminal alkynes in the presence of 1,8-diazabicyclo [5.4.O] undec-7-ene and tetrahydrofuran have been investigated as well.
- Nouzarian, Mahboobe,Hosseinzadeh, Rahman,Golchoubian, Hamid
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supporting information
p. 2913 - 2925
(2013/09/02)
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- Development of a regioselective N-methylation of (benz)imidazoles providing the more sterically hindered isomer
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An efficient and highly regioselective N-methylation of (NH)-(benz)imidazoles furnishing the sterically more hindered, less stable, and usually minor regioisomer has been developed. The methodology involves very mild reaction conditions and tolerates a wide range of functional groups.
- Van Den Berge, Emilie,Robiette, Raphael
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p. 12220 - 12223
(2014/01/06)
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- A convenient synthesis of 1,4-disubstituted imidazoles
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An efficient method for the regioselective protection of 4-alkyl-, 4-iodo, 4-vinylimidazoles has been developed via an alkylation-isomerization sequence with various imidazole-protecting groups. The initially formed mixture of 4/5-alkyl-, 4/5-iodo, and 4/5-vinylimidazoles are isomerized to the corresponding 4-isomers on treatment of a DMF solution with a small amount of RX and heating at 75°C.
- He, Yong,Chen, Yingzhong,Du, Hongwang,Schmid, Lesley A.,Lovely, Carl J.
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p. 5529 - 5532
(2007/10/03)
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- Novel farnesyl protein transferase inhibitors as antitumor agents
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Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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- Synthesis of chiral pilocarpine analogues via a C-8 ketone intermediate.
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The synthesis of a chiral pilocarpine analogue 3 in which the lactone ring is replaced by an oxazolidinone and the bridging methylene group is in the ketone oxidation state has been accomplished. The utility of this compound as a key intermediate for the preparation of more complex structures was demonstrated by its reduction to two alcohol epimers and its reaction with a methylene ylide.
- Holden, Kenneth G,Mattson, Matthew N,Cha, Kyung Hoi,Rapoport, Henry
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p. 5913 - 5918
(2007/10/03)
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- An efficient route to 5-iodo-1-methylimidazole: Synthesis of xestomanzamine A
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An efficient and practical route to C-5 functionalized N-methylated imidazoles is reported. 5-Iodo-1-methylimidazole was synthesized in four steps from imidazole, with complete regiospecificity, in 73% overall yield. The synthesis of xestomanzamine A, a marine natural product isolated in 1995 from an Okinawan sponge of Xestospongia sp., has been achieved using 5-iodo-1-methylimidazole in a modified Grignard reaction with a β-carboline ester moiety, in an overall yield of 59% based upon imidazole and 53% based upon tryptamine.
- Panosyan,Still
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p. 1110 - 1114
(2007/10/03)
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- Metal-Halogen Exchange Reactions of Mono- and Poly-halogenoimidazoles
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4(5)-Bromoimidazole gave a mixture of 4- and 5-bromo-1-methylimidazole on treatment with 1 or 2 mol equiv. of n-butyl-lithium in ether or THF under various reaction conditions followed by addition of dimethyl sulphate. 5-Iodo and 2,4,5-tribromo-1-methylim
- Iddon, Brian,Lim, Bee Lan
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p. 735 - 739
(2007/10/02)
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