Development of a Scalable Synthesis of a Drug-Linker for ABBV-3373
ORGANIC PROCESS RESEARCH & DEVELOPMENT(2024)
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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关键词
antibody-drugconjugate,drug-linker,glucocorticoid
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