Process Development and GMP Production of a Potent NAE Inhibitor Pevonedistat

Armitage Ian; Elliott Eric L.; Hicks Frederick; Langston Marianne; McCarron Ashley; McCubbin Quentin J.; OBrien Erin; Stirling Matt; Zhu Lei

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Process Development and GMP Production of a Potent NAE Inhibitor Pevonedistat

机译：强大的NAE抑制剂Pevonedistat的工艺开发和GMP生产

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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, regioselective sulfamoylation using N-(tert-butoxycarbonyl)-N-[(triethylenediammonium)sulfonyl]azanide. The linear process, involving six solid isolations, has been carried out in multiple cGMP productions on 15-30 kg scale to produce pevonedistat in 98% (a/a) chemical purity and 25% overall yield.

机译：描述了一种新型NEDD8激活酶（NAE）抑制剂Pevonedistat（MLN4924）的实用合成。关键步骤包括对映体选择性合成包含三个手性中心的氨基二醇环戊烷中间体，以及使用N-（叔丁氧基羰基）-N-[（三亚乙基二铵）磺酰基]氮杂化物进行新颖的区域选择性氨磺酰化。在多个cGMP生产中，已进行了线性工艺，涉及六种固体分离，生产规模为15-30 kg，以化学纯度98％（a / a）和总收率25％的方式生产pevonedistat。

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《Organic process research & development》 |2015年第9期|共9页
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Armitage Ian; Elliott Eric L.; Hicks Frederick; Langston Marianne; McCarron Ashley; McCubbin Quentin J.; OBrien Erin; Stirling Matt; Zhu Lei;
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1. Process Development and GMP Production of a Potent NAE Inhibitor Pevonedistat [J] . Armitage Ian, Elliott Eric L., Hicks Frederick, Organic process research & development . 2015,第9期

机译：强大的NAE抑制剂Pevonedistat的工艺开发和GMP生产
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Process Development and GMP Production of a Potent NAE Inhibitor Pevonedistat

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