- Synthesis method of 6-iodo [1, 2, 3] triazolo [1, 5-a] pyridine
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The invention relates to a synthesis method of 6-iodo [1, 2, 3] triazolo [1, 5-a] pyridine. The synthesis method comprises the following steps: adding 600-800g of oxime and 3-4L of anhydrous tetrahydrofuran into a 10L reaction bottle, stirring, filtering, pulping a filter cake by using 2L * 3 recovered toluene, sequentially extracting mother liquor filtered for the first time from filtrate by three times, combining organic phases, washing by using 2L of saturated saline solution, concentrating under reduced pressure until the solution is dry, obtaining 750-800g of crude product, 7.5-8L of methanol and 70-85g of activated carbon, refluxing for 1 hour, filtering while hot, washing the filter residue with 0.5 L of hot methanol, concentrating the filtrate under reduced pressure to about 4 L, refrigerating in a freezer, and filtering to obtain the product. The product is obtained under the condition of no transition metal, and the method has the advantages of high reaction efficiency, rapidness, mild conditions, simple and easily available substrates, wide applicability, short reaction time, high yield and the like, and meanwhile, the post-treatment of the reaction is also very simple and convenient, the harm to experiment operators is reduced, and the method is environment-friendly and meets the requirements of green chemistry.
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Paragraph 0019; 0022-0042
(2021/05/08)
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- PYRAZOLES AND METHODS OF MAKING AND USING THE SAME
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The invention is based on the discovery that compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of formula I (I).
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