A practical and chromatography-free synthetic process to selective M₁ and M₄ muscarinic acetylcholine receptors agonist was developed and demonstrated on a several hundred gram scale. The key feature of this route is N,N-dimethylcarbamoylation of the anilinic nitrogen on the spiro 7-azaindoline structure via intermolecular migration of the N,N-dimethylcarbamoyl group. The resulting compound 1 was prepared in 43% overall yield with a chemical purity >99% via six steps starting with (2-chloropyridin-3-yl)acetonitrile.

中文翻译：

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选择性M ₁和M ₄毒蕈碱型乙酰胆碱受体激动剂的合成方法开发

开发了一种实用且无色谱法的选择性M ₁和M ₄毒蕈碱型乙酰胆碱受体激动剂合成方法，并在数百克规模上得到了证明。这条路线的关键特征是N，N-经由分子间的迁移对螺7氮杂二氢吲哚的结构氮anilinic的-dimethylcarbamoylation N，N-二甲基氨基甲基。从（2-氯吡啶基-3-基）乙腈开始的六个步骤，以43％的总收率制备了所得化合物1，化学纯度> 99％。