1477-50-5Relevant articles and documents
Improved preparation method of indole-2-formic acid as starting material of perindopril
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, (2021/07/10)
The invention discloses an improved preparation method of indole-2-formic acid by using perindopril as a starting raw material, which comprises the following steps: S1, taking 2-bromobenzaldehyde and ethyl acetate as raw materials, under the action of sodium ethoxide, carrying out Claisen-Schmidt condensation reaction to synthesize ethyl 2-bromocinnamate; s2, carrying out cyclization reaction on the ethyl 2-bromocinnamate in an amide solvent by using cuprous halide as a coupling catalyst and sodium azide as a nitrogen source to synthesize the indole-2-formic acid in one pot. According to the invention, 2-bromobenzaldehyde is used as a raw material for preparation, ethyl 2-bromocinnamate is firstly prepared, then cuprous halide is used as a coupling catalyst, sodium azide is used as a nitrogen source, cyclization reaction is carried out in an amide solvent, indole-2-formic acid is synthesized in one pot, and the HPLC content is 99% or above.
Preparation method of indole-2-formic acid derivative
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Paragraph 0030-0041, (2020/07/14)
The invention discloses a preparation method of an indole-2-formic acid derivative, wherein the preparation method comprises the steps: by using an oxazolone compound as a raw material, carrying out areaction in an organic solvent at the temperature of 70-150 DEG C under the action of alcohol, alkali and a catalyst, tracking by TLC until the raw material is completely reacted, and separating andpurifying the obtained reaction solution to obtain the indole-2-formic acid derivative. The technology is adopted, the target product indole-2-formic acid derivative is prepared by taking an oxazolonecompound as a raw material through one-pot reaction under the action of alcohol, alkali and a catalyst, so that direct conversion from an oxazolone ring to an indole ring is realized, reaction stepsand an intermediate process are reduced, and the method has the characteristics of cheap raw materials, environmental friendliness and the like, and is suitable for industrial production.
Visible-Light-Promoted Efficient Aerobic Dehydrogenation of N-Heterocycles by a Tiny Organic Semiconductor Under Ambient Conditions
Su, Chenliang,Yu, Kunyi,Zhang, Hanjie,Zhu, Yongfa
supporting information, p. 1956 - 1960 (2020/04/10)
An efficient reusable catalytic system has been developed based on perylene diimide (PDI) organic semiconductor for the aerobic dehydrogenation of N-heterocycles with visible light. This practical catalytic system without any additives proceeds under ambient conditions. The minute aggregates of PDI molecules on the surface of SiO2 nanospheres form tiny organic semiconductors, resulting in high-efficiency photo-oxidative activity. Notably, the robustness of this method is demonstrated by the synthesis of a wide range of N-heteroarenes, gram-scale experiments as well as reusability tests.