CN105330643B — 卡比替尼的制备方法
Assigned to Harbin Yida Pharmaceutical Ltd By Share Ltd · Expires 2017-12-05 · 8y expired
What this patent protects
本发明揭示了一种卡比替尼(Cobimetinib，XL518，GDC‑0973)(I)的制备方法，其制备步骤包括：以(2S)‑2‑哌啶甲酸为原料，经酰腈化、水解、酯化和Boc保护制得中间体[2‑氧代‑2‑((2S)‑1‑叔丁氧羰基哌啶‑2‑基)]乙酸酯，该中间体经加成反应、还原反应和环合反应制得中间体(2S)‑1‑叔丁氧羰基‑2‑(3‑羟基氮杂环丁烷‑3‑基)哌啶，继而与侧链发生缩合反应制得卡比替尼(I)。该制备方法原料易得，工艺简洁，经济环保，适合工业化生产。
USPTO Abstract
本发明揭示了一种卡比替尼(Cobimetinib，XL518，GDC‑0973)(I)的制备方法，其制备步骤包括：以(2S)‑2‑哌啶甲酸为原料，经酰腈化、水解、酯化和Boc保护制得中间体[2‑氧代‑2‑((2S)‑1‑叔丁氧羰基哌啶‑2‑基)]乙酸酯，该中间体经加成反应、还原反应和环合反应制得中间体(2S)‑1‑叔丁氧羰基‑2‑(3‑羟基氮杂环丁烷‑3‑基)哌啶，继而与侧链发生缩合反应制得卡比替尼(I)。该制备方法原料易得，工艺简洁，经济环保，适合工业化生产。
Drugs covered by this patent
Bibliographic data sourced from FDA Orange Book + USPTO public records. Plain-English summary generated by AI grounded in source text. Patent term extensions (PTR, SPC, pediatric) may shift the effective expiry. Not legal advice.
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