85328-35-4Relevant articles and documents
Novel method for synthesizing 3-oxacyclobutanol
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Paragraph 0016; 0017; 0020; 0021; 0024; 0025, (2019/02/19)
The invention provides a novel method for synthesizing 3-oxacyclobutanol. The novel method is characterized in that epoxy chloropropane and glacial acetic acid are taken as raw materials, a catalyst is used for catalyzing the ring-opening reaction; under an organic strong acid condition, vinyl ethyl ether is added to perform upper protecting group reaction; under a strong-alkaline condition, ring-forming reaction is performed to obtain a key intermediate solution; the intermediate solution is extracted, concentrated and rectified to obtain an intermediate; catalysis amount of organic strong acid is used in the solvent by the intermediate to perform deprotection to obtain a 3-oxacyclobutanol crude product; the crude product is neutralized to be meta-alkalescent with weak alkaline, and is concentrated and rectified to obtain the 3-oxacyclobutanol product. The novel method has the characteristics of being cheap in raw materials, short in route, free of dangerous reagent, avoiding use of dangerous chemicals such as diazomethane, butyl lithium or 1,3-dichloroacetone, so that the synthesis method for 3-oxacyclobutanol can be safely amplified, and therefore, large-scale production can beperformed; and moreover, the 3-oxacyclobutanol is low in price, and is convenient to popularize.
3-oxetanone synthesis method
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Paragraph 0024; 0027; 0030, (2019/05/04)
The invention provides a 3-oxetanone synthesis method, which comprises: removing the protection group from an intermediate in an organic solvent I by using an organic strong acid, neutralizing with aweak alkali to achieve an alkaline pH value, carrying out concentration distillation on the solvent to obtain a oxetan-3-ol crude product, oxidizing the oxetan-3-ol with an oxidizing agent in the presence of a catalyst I, a halide and an alkali, and carrying out separating purification to obtain the 3-oxetanone product, wherein the intermediate preparation method comprises: carrying out a ring opening reaction by using epichlorohydrin and glacial acetic acid as raw materials under the catalysis of a catalyst II, adding ethyl vinyl ether under an organic strong acid condition, carrying out a protection group forming reaction, and carrying out a ring formation reaction under a strong alkali condition so as to obtain the key intermediate solution. According to the present invention, the oxetan-3-ol preparation process is combined without the purifying of oxetan-3-ol so as to eliminate the oxetan-3-ol purifying step; and the method has characteristics of inexpensive raw materials, short route, no use of dangerous reagents and the like.
NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
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Page/Page column 81, (2008/06/13)
Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n-Z-(CH2)m—PO(OR7)(OR8), —(CH2)nZ-(CH2)m—PO(OR7)Rg, —(CH2)n-Z-(CH2)m—OPO(OR7)Rg, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10);R5 and R6 are independently selected from H, alkyl and halogen;Y is R7(CH2)s or is absent; andX, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
