167145-13-3Relevant articles and documents
Preparation method of sarpogrelate hydrochloride intermediate
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, (2017/11/29)
The invention discloses a preparation method of sarpogrelate hydrochloride intermediate (2-hydroxy-3'-methoxy diphenylethane). According to the preparation method, m-bromoanisole, ethane, and o-benzyloxybromobenzene are taken as initial raw materials, an inorganic base is taken as an auxiliary agent, a palladium catalyst is adopted for catalysis, and o-benzoxy-3'-methoxy toluylene is obtained via reaction; o-benzoxy-3'-methoxy toluylene is subjected to hydrogenation debenzylation so as to obtain 2-hydroxy-3'-methoxy diphenylethane. The raw materials are common chemical raw materials, are cheap, and are high in safety; separation of by-products obtained in reaction process is relatively simple; separation is complete; steps are few; on-pot-method is adopted; and product yield is increased.
Synthetic method of sarpogrelate intermediate 2-[2-(3-methoxyphenyl)ethyl]phenol
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Paragraph 0008; 0013, (2016/11/02)
The invention discloses a synthetic method of a sarpogrelate intermediate 2-[2-(3-methoxyphenyl)ethyl]phenol and relates to the technical field of organic synthesis. In the method, with m-methoxyl chlorobenzene, which is easy to obtain and is low in cost, as a raw material, the method includes the steps of: 1) performing condensation to the raw material with triethyl phosphite; and 2) performing condensation with o-phenylmethoxyl benzaldehyde (which is prepared from salicylic acid and chlorobenzene), performing hydrogenation to alkylate a double bond, and crystallizing a product with petroleum ether to prepare a white crystal target product. The method simplifies process steps, reduces loss ratio and is 99.5% in product purity. The 2-[2-(3-methoxyphenyl)ethyl]phenol is used for preparing sarpogrelate hydrochloride, wherein single impurity is less than 0.1% in content and the product purity reaches more than 99.8%.
SAR study on arylmethyloxyphenyl scaffold: Looking for a P-gp nanomolar affinity
Nesi, Giulia,Colabufo, Nicola Antonio,Contino, Marialessandra,Perrone, Maria Grazia,Digiacomo, Maria,Perrone, Roberto,Lapucci, Annalina,Macchia, Marco,Rapposelli, Simona
, p. 558 - 566 (2014/04/03)
Starting from the previously developed P-gp ligands 1a and 1b (EC 50 = 0.25 μM and 0.65 μM, respectively), new arylmethyloxyphenyl derivatives have been synthesized as P-gp modulators in order to investigate: (i) the effect of small electron-do