连接器
可扩展性
化学
计算机科学
光学
材料科学
物理
操作系统
作者
Nathan B. Bennett,Bradley D. Gates,Justin A. Simanis,James W. Treadway,Steven M. Richter,Dennie S. Welch
标识
DOI:10.1021/acs.oprd.3c00447
摘要
A scalable process to produce glucocorticoid-bearing drug-linker 1, utilized in the conjugation with the monoclonal antibody (mAb) adalimumab, has been developed. The route improves upon the first-generation approach through a more convergent assembly of the linker and warhead. Optimization and insights into the key transformations are discussed, including a challenging acetonide deprotection, acetal formation under strongly acidic conditions, and amide coupling and purification.
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