《Synthesis of the major isomers of Aprepitant and Fosaprepitant》.pdf

ChineseChemicalLetters24(2013)1118-1122 ContentsIistsava_IableatScienceDirect ChineseChemicalLetters journaIhomePage：WWW．eIsevier．com ／Iocate／ccIet Originalarticle SynthesisofthemajorisomersofAprepitantandFosaprepitant ⑩cross W ei—LiW an ，YunHeaMeiGuanbXiao—LongLiaXUCheng ．YongWu ’ ， KeyLaboratoryofDrugTargetingandDrugDeliverySystemoftheEducationMinistry，Department MedicinalChemistry，WestChinaSchoolofPharmacy Sichuon University．Chengdu610041，China WestChinaHospita1．SichuanUniversiyt，Chengdu610041，China A RT IC LE IN F0 A B ST R A C T Articlehistory： ThesynthesisoftwoisomersofAprepitant(APT)andthreeisomersofFosaprepitant(FPT)，crucial Received 13 May2013 componentsforqualitycontro¨nmanufacturing．isdescribed．Herein．threechiralcentersintheisomers Receivedinrevisedform 3July2013 ofAprepitantareestablishedinhighyieldbyinducedcrystallizationandchiralreduction．Additionally． Accepted10July2013 the isomersofAprepitantare utilized t0 synthesize the isomersofFosaprepitantwith the same Availableonline18September2013 stereochemistry．AI1thetargetcompoundswereconfirmedbyelementa1analyses．1R．NMRandMSdata analysis． Keywords： @ 2013YongW u．PublishedbyElsevierB．V．onbehalfofChineseChemicalSociety．AIlrightsreserved． AprepitantandFosaprepitant Majorisomers Chemicalsynthesis 1．Introduction Theofrmationoftheset