77435-44-0Relevant articles and documents
Stable isotope-labeled sulfadimidine and synthesis method thereof (by machine translation)
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Paragraph 0034; 0037; 0040; 0044; 0047, (2019/08/01)
The invention discloses a stable isotope-labeled sulfadimidine and a synthesis method. S1: The stable isotope-labeled acetaminophthic acid chloride; S2: the stable isotope-labeled p-acetyl aminobenzyl chloride is prepared; and the stable isotope-labeled p-acetyl aminobenzyl chloride is reacted, 2 -dimethyl -4 -5 - 6 -bromopyrimidine, and the like. S3 is obtained by reacting the stable isotope-labeled acetaminophthyl chloride with chlorosulfonic acid. The formed intermediate is hydrolyzed under basic conditions to prepare a stable isotope-labeled sulfadimidine. Compared with the prior art, the method has the advantages of mild conditions, simple process, short process route, easy separation and purification of products, high yield, high chemical purity and stable isotope abundance of 99% the obtained products, and high use value, and can be used as a standard reagent for quantitatively detecting sulfadimethoxuracil; and the method has good economical. (by machine translation)
Stable isotope labeled sulfamethoxazole and synthesis method thereof
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Paragraph 0035; 0040; 0045; 0048, (2019/07/29)
The invention discloses stable isotope labeled sulfamethoxazole and a synthesis method thereof. The synthesis method comprises following steps: S1, stable isotope labeled aniline and acetic anhydrideare subjected to a reaction, and stable isotope labeled acetaminobenzene is prepared; S2, stable isotope labeled acetaminobenzene and chlorosulfonic acid are subjected to a reaction, and stable isotope labeled p-acetamidobenzene sulfonyl chloride is prepared; S3, stable isotope labeled p-acetamidobenzene sulfonyl, 3-amino-5-methylisoxazole and 4-dimethylaminopyridine are subjected to a reaction, and stable isotope labeled acetylsulfamethoxazole is prepared; S4, stable isotope labeled acetylsulfamethoxazole is hydrolyzed under the alkaline condition, and stable isotope labeled sulfamethoxazoleis obtained. The synthesis process is simple, a product is easy to separate and purify, chemical purity and isotope abundance of the obtained product both reach 99% or higher, and the product meets the requirement of a standard reagent for quantitatively detecting sulfamethoxazole; stable isotope labeled sulfamethoxazole has high use value and good economic efficiency.
Stable isotope deuterium labeled sulfanilamide drug and preparation method thereof
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, (2018/04/26)
The invention belongs to the technical field of chemical synthesis, and specifically relates to a stable isotope deuterium labeled sulfanilamide drug and a preparation method thereof. The preparationmethod comprises the following steps: (1) subjecting benzene-d6 (I) to a nitratlon reaction so as to prepare deuterium labeled nitrobenzene-d5 (II); (2) reducing nitro of the deuterium labeled nitrobenzene-d5 (II) so as to prepare deuterium labeled aniline-d5 (III); (3) under the conditions of anhydrous sodium acetate and glacial acetic acid, subjecting the deuterium labeled aniline-d5 (III) and acetic anhydride to a reaction so as to prepare deuterium labeled N-acetanilide-d5 (IV); (4) subjecting the deuterium labeled N-acetanilide-d5 (IV) and chlorosulfonic acid to a reaction so as to prepare deuterium labeled 1-chlorosulfonyl-4-acetamidobenzene-d4 (V); and (5) allowing R to substitute chlorine of the deuterium labeled 1-chlorosulfonyl-4-acetamidobenzene-d4 (V), and carrying out hydrolysis so as to prepare an isotope deuterium labeled sulfanilamide drug (VII). The preparation method provided by the invention has the advantages of simple reaction conditions, short reaction time, highconversion efficiency, strong economy, and applicability to mass synthesis.
Synthesis of deuterium-labelled fosamprenavir calcium
Shi, Lei,Chen, Liping,Chen, Ryan,Chen, Liqin
experimental part, p. 148 - 152 (2011/07/31)
This study describes the synthesis of deuterium-labelled fosamprenavir calcium. The stable isotopic-labelled compound was prepared starting from L-phenylalanine in 18 steps with a 9% overall yield. Copyright
