1918-77-0Relevant articles and documents
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Blanchette,Brown
, p. 1066 (1952)
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Method for efficiently preparing thiophene medical intermediates
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Paragraph 0014; 0016; 0018, (2021/05/29)
The invention belongs to the field of synthesis of thiophene medical intermediates, discloses a method for efficiently preparing the thiophene medical intermediates, and particularly discloses a process for synthesizing 2-thiopheneacetic acid from 2-thiopheneethanol through a catalytic reaction, catalyzing the 2-thiopheneacetic acid to generate a 2-thiopheneacetyl chloride crude product and then purifying the 2-thiopheneacetyl chloride crude product. The reaction conditions are mild, the product purity is high, the synthesis efficiency is high, and the yield reaches 90% or above.
Oxidation of Alkynyl Boronates to Carboxylic Acids, Esters, and Amides
Li, Chenchen,Li, Ruoling,Zhang, Bing,Zhao, Pei,Zhao, Wanxiang
supporting information, p. 10913 - 10917 (2020/05/25)
A general efficient protocol was developed for the synthesis of carboxylic acids, esters, and amides through oxidation of alkynyl boronates, generated directly from terminal alkynes. This protocol represents the first example of C(sp)?B bond oxidation. This approach displays a broad substrate scope, including aryl and alkyl alkynes, and exhibits excellent functional group tolerance. Water, primary and secondary alcohols, and amines are suitable nucleophiles for this transformation. Notably, amino acids and peptides can be used as nucleophiles, providing an efficient method for the synthesis and modification of peptides. The practicability of this methodology was further highlighted by the preparation of pharmaceutical molecules.
Preparation method of 2-thiopheneacetyl chloride
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Paragraph 0034-0037; 0041-0044; 0046-0049; 0051-0054; 0056, (2020/08/30)
The invention discloses a preparation method of 2-thiopheneacetyl chloride, and belongs to the technical field of chemical synthesis. The preparation method comprises the following steps: (1) dissolving 2-thiopheneethanol in an organic solvent, and reacting at 50-120 DEG C under the action of a solid acid catalyst, an alkali and an oxidant to prepare 2-thiopheneacetic acid, wherein the oxidant isoxygen or hydrogen peroxide; and (2) dissolving 2-thiopheneacetic acid in an organic solvent, and dropwise adding thionyl chloride to carry out an acylating chlorination reaction by taking an alkalineionic liquid as a catalyst so as to prepare 2-thiopheneacetyl chloride. The preparation method is simple in route, easy in obtaining of raw materials, mild in reaction conditions, and capable of realizing few byproducts and easy purification and separation due to adoption of oxygen or hydrogen peroxide as the oxidant in synthesis of 2-thiopheneacetic acid; and when the acylating chlorination reaction of 2-thiopheneacetic acid is carried out, the basic ionic liquid is adopted as the catalyst, the reaction process is stable and easy to control, the product yield is high, few byproducts are produced, so the method is an efficient and green synthesis process.