With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5264-35-7,5-Methoxy-3,4-dihydro-2H-pyrrole,as a common compound, the synthetic route is as follows.
5264-35-7, EXAMPLE I 5-Amino-2,3-dihydro-1H-indolizin-7-one Monohydrochloride To a solution of lithium diisopropylamide (LDA), prepared from n-BuLi (125 ml, 0.2M) and diisopropylamine (20.24 g, 0.2M), in dry THF (200 ml) was added under N2 at -10¡ã C. 5-methylisoxazole (8.31 g, 0.1 M). The resultant yellow suspension was stirred at -10¡ã C. for 1 hr before 1-aza-2- methoxy-1-cyclopentene (9.9 g, 0.1M) was added dropwise. A light yellow precipitate was immediately formed. The mixture was allowed to warm to ambient over a period of 19 hr. MeOH (100 ml) was slowly added with external cooling so that the internal temperature remained at 25¡ã-26¡ã C. The resulting reddish solution was then stirred at ambient for 24 hr and evaporated in vacuo. Flash column chromatography (30percent MeOH in CH2 Cl2 on silica gel, Em-60) followed by recrystallization (MeOH/Et2 O) gave the desired free base (3 g, 20percent); mp> 230¡ã C. It was then transformed into its HCl salt in MeOH with conc HCl. The salt was further recrystallized from MeOH/Et2 O to yield the title compound; mp>250¡ã C. yield 3 g, 81percent); TLC (30percent MeOH in CH2 Cl2); Rf=0.37; IR (KBr) cm-1, 3500, 3140, 1670, 1590. Anal. Calcd for C8 H10 N2 O. HCl: C, 51.48; H, 5.94; N, 15.01. Found: C, 51.08; H, 5.77; N, 14.89.
The synthetic route of 5264-35-7 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; Ortho Pharmaceutical Corporation; US4602013; (1986); A;,
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