发明名称 ENANTIOMERIC SEPARATION AND PURIFICATION OF 2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-4-CARBOXYLIC ACID AMIDE DERIVATIVES
摘要 A method for the purification of cyclic indole compounds that provides advantages over previously-known methods. Using the method of the present invention allows for the facile preparation of a good quality solid form of these compounds.
申请公布号 US2016168091(A1) 申请公布日期 2016.06.16
申请号 US201414905649 申请日期 2014.07.17
申请人 GE HEALTHCARE LIMITED 发明人 NILSEN Sondre;MANTZILAS Dimitrios
分类号 C07D209/84;A61K51/04;G01N33/60;C07D209/88 主分类号 C07D209/84
代理机构 代理人
主权项 1. A method comprising: separating an S-enantiomer from an R-enantiomer wherein said S-enantiomer and said R-enantiomer are provided in a racemic mixture and wherein each of said S-enantiomer and said R-enantiomer is a compound of Formula I: wherein: R1 is C1-4 alkylene-LG wherein LG is a leaving group; R2 is hydrogen, hydroxyl, halo, cyano, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl, or C1-3 fluoroalkoxy; R3 and R4 are independently C1-3 alkyl, C7-10 aralkyl, or R3 and R4, together with the nitrogen to which they are attached, form a nitrogen-containing C4-6 aliphatic ring optionally comprising 1 further heteroatom selected from nitrogen, oxygen and sulfur; Y1 is O, S, SO, SO2 or CH2; Y2 is CH2, CH2—CH2, CH(CH3)—CH2, CH2—CH2—CH2 or CH—(CH—CH2—CH—CH2)—CH; said variable bond is above the plane for the S-enantiomer and below the plane for the R-enantiomer as illustrated respectively in Formulas I-S and I-R: dissolving one of said separated enantiomers in a suitable organic solvent; precipitating said dissolved enantiomer out of the solution obtained in step (ii) wherein said precipitating step comprises addition of water; isolating the precipitate obtained in step (iii).
地址 Little Chalfont Buckinghamshire GB