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【结 构 式】 
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【分子编号】51174 【品名】4,5-dimethyl-2-pyrrolidinone 【CA登记号】 |
【 分 子 式 】C6H11NO 【 分 子 量 】113.15948 【元素组成】C 63.69% H 9.8% N 12.38% O 14.14% |
与该中间体有关的原料药合成路线共 2 条
合成路线1
该中间体在本合成路线中的序号：(I)The title compound was prepared by two related procedures. Treatment of cis-4,5-dimethyl-2-pyrrolidinone (I) with dimethyl sulfate gave the methoxypyrroline (II). The methoxy group of (II) was then displaced with dicyclopropylmethylamine (III) to provide the desired aminopyrroline.
| 【1】 Renard, P.; Feldman, J.; Bousquet, P.; Bruban, V.; Schann, S.; Scalbert, E.; Pfeiffer, B.; Ehrhardt, J.-D. (ADIR et Cie.); Aminopyrrolidine derivs., processes for their preparation and pharmaceutical compsns. comprising them. EP 1101756; FR 2801051; JP 2001139545; US 6300366 . |
合成路线2
该中间体在本合成路线中的序号：(I)In a more convenient method, pyrrolidinone (I) was converted to the thiolactam (IV) upon treatment with Lawesson's reagent. Alkylation of (IV) with iodomethane furnished the corresponding (S)-methyl derivative (V). This was finally condensed with dicyclopropylmethylamine (III), yielding the title compound.
| 【1】 Feldman, J.; Bousquet, P.; Pfeiffer, B.; Bruban, V.; Scalbert, E.; Renard, P.; Pompermayer, K.; Schann, S.; Ehrhardt, J.-D.; Synthesis and biological evaluation of pyrrolinic isosteres of rilmenidine. Discovery of cis-I-trans-dicyclopropylmethyl-(4,5-dimethyl-4,5-dihydro-3H-pyrrol-2-yl)-amine (LNP 509), an I1 imidazoline receptor selective ligand with hypotensive activity. J Med Chem 2001, 44, 10, 1588. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 51174 | 4,5-dimethyl-2-pyrrolidinone | C6H11NO | 详情 | 详情 | |
| (III) | 24691 | dicyclopropylmethanamine | C7H13N | 详情 | 详情 | |
| (IV) | 51176 | 4,5-dimethyl-2-pyrrolidinethione | C6H11NS | 详情 | 详情 | |
| (V) | 51177 | 2,3-dimethyl-3,4-dihydro-2H-pyrrol-5-yl methyl sulfide; 2,3-dimethyl-5-(methylsulfanyl)-3,4-dihydro-2H-pyrrole | C7H13NS | 详情 | 详情 |
Extended Information