- Preparation of Sulfamates and Sulfamides Using a Selective Sulfamoylation Agent
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Sulfamates and sulfamides are prevalent in biological molecules, but their universal synthetic methods are limited. We herein report a sulfamoylation agent with high solubility and shelf stability. Various sulfamates and sulfamides can be synthesized directly from alcohols or amines by employing this agent with high selectivity and high yields. This protocol was also successfully used for late-stage sulfamoylation of pharmaceuticals containing a hydroxyl or amino group.
- Wang, Hai-Ming,Xiong, Chao-Dong,Chen, Xiao-Qu,Hu, Chun,Wang, Dong-Yu
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supporting information
p. 2595 - 2599
(2021/05/05)
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- Catalytic Sulfamoylation of Alcohols with Activated Aryl Sulfamates
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We report a new catalytic method for alcohol sulfamoylation that deploys electron-deficient aryl sulfamates as activated group transfer reagents. The reaction utilizes the simple organic base N-methylimidazole, proceeds under mild conditions, and provides
- Rapp, Peter B.,Murai, Koichi,Ichiishi, Naoko,Leahy, David K.,Miller, Scott J.
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supporting information
p. 168 - 174
(2019/12/30)
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- Process Development and GMP Production of a Potent NAE Inhibitor Pevonedistat
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A practical synthesis of a novel NEDD8-activating enzyme (NAE) inhibitor pevonedistat (MLN4924) is described. Key steps include an enantioselective synthesis of an amino-diol cyclopentane intermediate containing three chiral centers and a novel, regiosele
- Armitage, Ian,Elliott, Eric L.,Hicks, Frederick,Langston, Marianne,McCarron, Ashley,McCubbin, Quentin J.,Obrien, Erin,Stirling, Matt,Zhu, Lei
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p. 1299 - 1307
(2015/09/28)
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- PREPARATION METHOD OF MLN4924 AS AN E1 ACTIVATING INHIBITOR
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The present invention relates to a method for preparation of MLN4924 as an E1 activating inhibitor, and more specifically, to a method for efficient and stereoselective preparation of MLN4924 by means of key steps involving stereoselective reduction of cy
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- Stereoselective synthesis of MLN4924, an inhibitor of NEDD8-activating enzyme
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MLN4924 (1), which is in clinical trials as an anticancer agent, was stereoselectively synthesized from d-ribose via a route involving stereoselective reduction, regioselective cleavage of an isopropylidene moiety, and selective displacement of a cyclic s
- Lee, Hyuk Woo,Nam, Soo Kyung,Choi, Won Jun,Kim, Hea Ok,Jeong, Lak Shin
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p. 3557 - 3561
(2011/06/25)
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- HYDROCHLORIDE SALT OF ((1S,2S,4R)-4-{4-[(1S)-2,3-DIHYDRO-1H-INDEN-1-YLAMINO]-7H-PYRROLO [2,3-D]PYRIMIDIN-7-YL}-2-HYDROXYCYCLOPENTYL)METHYL SULFAMATE
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Disclosed is a compound of formula (I); crystalline forms thereof, and solvates thereof; pharmaceutical compositions comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and a pharmaceutically acceptable carrier or diluent; and the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting an El activating enzyme, particularly NAE, including, e.g., cancer.
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Page/Page column 37-38
(2010/12/17)
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- Inhibitors of E1 activating enzymes
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This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
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Page/Page column 54
(2010/11/28)
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- INHIBITORS OF E1 ACTIVATING ENZYMES
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This invention relates to compounds that inhibit El activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
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Page/Page column 139
(2008/06/13)
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