H) ;13C 匪R(100MHz，CDCI3)S = 172.7， 170.7.166.1.140.0. 133.6.132.6.131.1.129.3.128.7.128.6.127.6.67.1.62.0.40.0, 36.7,14.l；HRMS(ESI)calcd for C20H20 204CI (M+H) +:387.1112,Found:387.1112；97:3 e.r.由HPLC[Chiralcel IA, 75:20:5 己烷/(己烷：i-PrOH: CH30H = 90:5:5)/i-Pr0H, 0 · 7mljmin)]测定，tr(major) = 136 · Omin, tr(minor) = 112 · 0min〇
实施例48: (2R，3S)_乙基I-苯甲酰氨基-3-(4-溴苯基）-5-氧代吡 咯烷-2-羧酸酯:yellow oil;[a]D23(c 2.49,012(:12)=-61.8°;? NMR(400MHz，CDCI3)6 = 1.21(t,J = 7.2Hz,3H) ,2.64(dd,J=17.6Hz,6.4Hz,1H) ,3.1(dd,J=17.6Hz,9.6Hz,1H), 3.56- 3.61(m,lH) ,4.15-4.26(m,2H) ,4.68(d ,J = 5.6Hz , 1H), 7.34-7.54(m, 7H), 7.84(d J = 7.2Hz，2H)，9.49(bs，lH);13C NMR(100MHz，CDCI3)S = 173.4，170.7，166.0，140.4，132.5， 132.2.130.9.129.0. 128.6.127.6.121.7.67.1.62.0.40.1.36.8.14.1;HRMS(ESI)calcd for C2oH2〇2〇4Br+:431.0606，Found:431.0606;97:3 e.r.由HPLC[Chiralcel IA,75:20:5 己烧/(己烧：i-PrOH:CH30H=90:5:5)/i-Pr0H，0 ·7mL/min)]测定，tr(major) = 142·7min, tr (minor) = 118.4min〇
实施例49: (2R，3S)_乙基I-苯甲酰氨基-5-氧代-3-(对甲苯基））吡 咯烷-2-羧酸酯:黄色油；[a]D23(c 2 ·41 ,CH2CI2) =_46 · 8° ; 1H NMR(400MHz，CDCI3)6 = 1 · 22 (t,J = 7.2Hz,3H) ,2.36(s,3H) ,2.65(dd,J= 17.6Hz,9.6Ηζ,1Η) ,3.02(dd J= 17.6Hz, 9.6Hz,lH) ,3.53-3.59(m,lH) ,4.15-4.28(m,2H) ,4.70(d,J = 6.0Hz, 1H) ,7.20(d,J = 7.6Hz,2H) ,7.35-7.44(m,4H) ,7.53(t,J = 7.2Hz,lH) ,7.85(d,J = 7.2Hz,2H) ,8.67(bs, 1H) ;3C 匪R(100MHz，CDCI3)S = 172.9,171.0,166.0,138.3,137.4,132.5,131.3,129.8， 128·7，127·6，127·I，67·4，61·9，40·3，36·8，21·I，14·I;HRMS(ESI)calcd for C2iH232〇4(M +H) + :367.1658，Found:367.1657;97:3 e.r.由HPLC[Chiralcel IA，75:20:5己烷/(己烷： i-PrOH: CH30H = 90: 5:5)/i-Pr0H，0 · 7mL/min)]测定，tr(major) = 108 · Imin，tr(minor)= 86.Omin。
实施例50: (2R，3S)_乙基I-苯甲酰氨基-3-(4-甲氧基苯基)-5-氧 代吡咯烷-2-羧酸酯：黄色油；[a)D23(c 2.2，CH2CI2)=-69.9° !1H NMR(400MHz，CDCI3) ￡ = 1.23(t ,J = 7.2Hz,3H),2.65(dd ,J=18.0Hz,6.8Hz,lH),2.99(dd ,J=17.6Hz,9.6Hz,lH), 3.51-3.57(m,lH) ,3.82(s,3H) ,4.16-4.29(m,2H) ,4.68(d,J = 5.6Hz,lH) ,6.93(d,J = 8.8Hz,2H) ,7.39-7.47(m,4H) ,7.55(t,J = 7.2Hz,lH) ,7.85(d,J = 7.2Hz,2H) ,8.42(bs, 1H);13C NMR(100MHz,CDCI3M = 172.6,171.0,166.0,159.1,133.5,132.6,131.4,128.8， 128.2,127.5,114.5,67.5,61.9,55.3,39.9,36.8,21.8,14.2；HRMS(ESI)calcd for C2iH23N205(M+H) +:383·1607,Found:383·1608;97:3 e·r·由HPLC[Chiralcel IA,70:20:10 己烧/(己烧/i-PrOH: CH30H = 90:5:5)/i-Pr0H,0 · 7mL/min)]测定，tr(ma jor) = 82 · 2min，tr (minor) =73 · 0min〇
实施例51: (2R，3S)_乙基I-苯甲酰氨基-3-(萘-I-基)-5-氧代 吡咯烷-2-羧酸酯：黄色油；[a]D23(c 2.08，CH2CI2)=-11.1° !1H 匪R(400MHz，CDCI3)S = 1.15(t ,J = 7.2Hz,3H),2.79(dd ,J=17.2Hz,5.6Hz,lH),3.21(dd ,J=17.6Hz,5.6Hz,lH), 4.16-4.26(m,2H),4.43-4.48(m,lH),5.02(d ,J = 4.8Hz,lH),7.44(t ,J = 7.6Hz,2H),7.52- 7.61(m，4H)，7.83-7.94(m，5H)，8· ll(d，J = 8.4Hz，lH)，8.70(bs，lH) ;13C 匪R(100MHz， CDCI3W = 172.8,171.3,166.2,136.8,134.1,132.6,131.4,130.9,129.3,128.7,128.3， 127.6,126.6,126.0,125.8,122.6,66.4,62.1,36.3,14.0；HRMS(ESI)calcd for C24H23N2〇4(M+H) + :403.1658，Found:403.1659;97:3 e.r.由HPLC[Chiralcel IA，90: 10hexanes/i_Pr0H，0 · 7mL/min)]测定，tr(major) = 93.4min，tr(minor) = 78 · 9min〇
实施例52: (2R，3R)_乙基I-苯甲酰基-3-(呋喃-2-基）-5-氧代吡咯 烷-2-羧酸酯：无色油；[a]D23(c 1.55，CH2Cl2)=-40.8° !1H NMR(400MHz，CDCI3)S = 1.26(t， J = 7.2Hz，3H)，2.80-2.95(m，2H)，3.74(dd，J= 15·2Ηζ，7·2Ηζ，1Η)，4· 19-4.31(m，2H) ,4.80 (d，J = 6.4Hz，lH)，6.36-6.39(m，2H)，7.43(t，J = 7.6Hz，3H)，7.53(t，J = 7.6Hz，lH) ,7.83 (d，J = 7.6Hz，2H)，8.48(bs，lH);13C 匪R(100MHz，CDCI3)S = 172.1，170.4，165.8，152.5， 142.4,132.6,131.3,128.7,127.5,110.6,106.8,64.7,62.1,34.4,33.6,14.1;HRMS(ESI) calcd for Ci8Hi9N2〇5(M+H)+:343.1294，Found:343.1295;95:5 e.r.由HPLC[Chiralcel 1八，70:20:10己烷/(己烷：卜卩抑!1:013011=90:5:5)八^^0!1，0.71111711^11)]测定，一(1^]_(^)= 63·7min，tr(minor) = 56·4min 〇
实施例53: (2R，3S)_乙基]-苯甲酰氨基-3-(3-(环戊氧基)-4- 甲氧基苯基)-5-氧代吡咯烷-2-羧酸酯:黄色油；[a]D23(c 0.63，CH2CI2) =-66.3° ; 1H NMR (400MHz,CDCI3)5 = 1.24(t,J = 7.2Hz,3H), 1.61-1.63(m,2H) ,1.86-2.02(m,6H),2.63(dd, J=17.2Hz,6.0Hz,lH) ,2.99(dd,J=17.2,6.0Hz,lH) ,3.48-3.53(m,lH) ,3.85(s,3H), 4.18-4.29(m,2H) ,4.69(d ,J = 4.8Hz , 1H) ,4.90-4.92(m, 1H) ,6.86(d ,J = 8. OHz , 1H) ,6.96 (d ,J = 8.0Hz,lH) ,7.06(s,lH),7.46(t ,J = 7.6Hz,2H) ,7.56(t ,J = 7.6Hz , 1H) ,7.84(d J = 7.2Hz，2H)，8.28(bs，lH);13C NMR(100MHz，CDCI3)S = 173.1，171.0，166.1，150.7，147.3， 134.2,132.5,128.6,127.6,119.3,115.1,110.7,80.6,67.5,51.9,56.4,40.2,36.9,32.9, 24.1,14.2,；HRMS(ESI)calcd for C26H3iN206(M+H) +:467.2182,Found:467.2813；96:4 e · r ·由HPLC(Chiralcel IA, 93 :7己烧/i-PrOH, 0 · 7mL/min)测定，tr(ma jor) = 94 · 6min，tr (minor) =73· lmin〇
实施例54: (2R，3S)_乙基1-(4-氯代苯甲酰)-5-氧代-3-苯基吡咯 烷-2-羧酸酯：白色固体，trans:cis = 7:l，两种异构体的产率70%;[a]D23(c 1.25，CH2CI2) = -26.8° .1H NMR(400MHz，CDCI3)S = 1.22(t，J = 7.2Hz，3H)，2.72(dd，J=17.6Hz，6.8Hz， 1H)，3.09(dd，J=17·6Ηζ，9·6Ηζ，1Η)，3.59-3.64(m，lH),4.15-4.28(m，2H)，4.70(d，J= 5.6Hz，1H)，7.32-7.48(m，7H)，7.77(d，J = 8.8Hz，2H)，9.19(bs，1H) ;3C NMR(100MHz,CDCI3) 8-73.4,170.8,164.9,141.2,129.2,129.0,128.9,127.8,127.2,67.3,61.9,40.6,36.8, 14.1;HRMS(ESI)calcd for C2oH2o 2〇4CI(+H)+:387.1112，Found:387.1111;96:4 e.r.由 HPLC[Chiralcel 1厶，73:20:7己烷/(己烷：卜卩抑!1:(：!13011 = 90:5:5)八-?抑!1，0.71111711^11)] 测定，tr(major) = 125 · 9min，tr(minor) = 100 · Omin0
实施例55: (2R，3S)_乙基1-(4-氟苯甲酰氨基)-5-氧代-3-苯基吡咯 烷-2-羧酸酯：白色固体，trans : ci s = 5:1，两种异构体的产率61 % ; [0 ]D23 (c 1.0，CHCI3) =-59.6;? NMR(400MHz，CDCI3)S9.19(s，1H),7.89-7.86(m，2H),7.50-7.40(m，4H),7.35-7.27(m,lH) ,7.09-7.01(m,2H) ,4.72(d ,J = 5.6Hz ,H), 4.36-4.10(m, 2H), 3.65-3.60(m, lH),3.10(dd ,J=17.6,10.0Hz,lH),2.93(dd ,J = 17.2,6.4Hz,lH),1.22(t ,J = 7.2,3H)；13C 匪R(100MHz，CDCI3)6173.6,171.0,166.8,165.0,164.3,141.5,130.3((1, J = 9.0Hz), 129.3,128.0,127.5(d J= 13.0Hz) ,116.0(d,J = 22.0Hz) ,69.6,62.1,40.8,37.0.14.3； HRMS forC20H20N204[M+l!+Calculated:371·1407,Found:371·1398;96:4 e·r·由HPLC [Chiralcel 1厶，75:20:5己烷/(己烷：卜卩抑!1:013011=905:5)八^^0!1，0.71111711^11)]测定，一 (major) = 146·8min，tr(minor) = 111 ·6min〇
实施例56: (2R，3S)_乙基1-(3-溴苯甲酰氨基)-5-氧代-3-苯基吡 咯烷-2-羧酸酯：白色固体，trans: cis = 5:1，两种异构体的产率59% ; [a]D23(c 1 · I ,CHCI3) = -45.3;? NMR(400MHz，CDCI3)S9.09(s，1H)，7.97(s，1H)，7.77((1, J = 8.0Hz，lH)，7.65((1, J = 8.4Hz，lH)，7.47(d，J = 7.6Hz，2H)，7.40(t，J = 7.6Hz，2H)，7.34-7.26(m，2H)，4.71(d，J =5·6Ηζ，1H)，4.31-4.09(m，2H),3.63-3.58(m，lH)，3.06(dd，J=17.2,9·6Ηζ，1Η),2.70 (dd，J=17.6,6.8Hz，lH)，1.22(t，J = 7.2,3H) ;13C 匪R(100MHz，CDCI3)6173.3，171.0， 164.7,141.5,135.6,133.2,131.1,130.4,129.3,127.9,127.4,126.2,123.1,67.4,62.2, 40.8,36.9,14.3；HRMS for C2〇H2oN204Br[M+l!"Calculated:431.0606,Found:431.0609； HPLC analysis :96 :4 e.r.由HPLC[Chiralcel IA,75 :20 :5 己烷/(己烷：i-PrOH: CH3OH = 90:5:5)/i_Pr0H，0 · 7mL/min)]测定，tr(major) = 47.4min, tr(minor) = 52 · 9min〇
实施例57: (2R，3S)_乙基1-(4-甲氧基苯甲酰氨基)-5-氧代-3- 苯基吡咯烷-2-羧酸酯：白色固体，trans: cis = 5:1，两种异构体的产率70% ; [a]〇23(c 0.3， 003)=-58.3;? NMR(400MHz，CDCI3)68.44(s，H) ,7.81-7.79(m，2H)，7.47((1, J = 7.6Hz， 2H) ,7.39( t,J = 7.2Hz,2H), 7.32-7.25(m,lH), 6.93-6.88(m,2H) ,4.71 (d ,J = 5.6Hz , 1H), 4.29- 4.10(m,2H),3.84(s,3H),3.59-3.54(m,lH),3.02(dd,J=17.6,10.0Hz,lH),2.67 (dd，J=17.6,6.8Hz，lH)，1.20(t，J = 7.2,3H) ;3C 匪R(100MHz，CDCI3)S173.0，171.2， 165.8,163.3,141.7,129.7,129.3,127.9,127.4,123.8,114.2,67.5,62.1,55.7,40.8， 37.0. 14.4；HRMS for C2iH23N205[M+1 !"Calculated:383.1607,Found:383.1637；HPLC analysis: 97: 3 e · r ·由HPLC[Chiralcel IA, 65: 30 :5己烷/(己烷：i-PrOH: CH30H=90: 5: 5)/i-Pr0H,0 · 7mL/min)]测定，tr(major) = 96 · 6min, tr(minor) = 103 · Omin0
实施例58:(2R，3S)_乙基l-{4-溴苯甲酰氨基)-5-氧代-3-苯基吡 略烧-2-羧酸酯:White solid，trans : cis = 5 :1，两种异构体的产率65% ; [a]o23(c 0.2， 01(313)=-10;? 匪R(400MHz，CDCI3)68.91 (s，lH)，7.68((1, J = 8.4Hz，2H)，7.53((1, J = 8.4Hz,2H) ,7.46(d ,J = 7.6Hz,2H),7.39-7.25(m,3H) ,4.69(d ,J = 5.6Hz , 1H), 4.29-4.10 (m,2H),3.62-3.56(m,lH) ,3.05(dd,J=17.6,9.6Hz,lH) ,2.69(dd,J=17.6,6.4Hz,lH), 1.21(t，J = 7.2,3H);13C NMR(100MHz，CDCI3)6173.2，171.0，165.3，141.5，132.2，130.2， 129.4.129.3.128.0. 127.7.127.4.67.5.62.2.40.8.36.9.14.3；HRMS for C20H20 204Br[M + 1]+Calculated:431.0606,Found:431.0626;95:5 e.r.由HPLC[Chiralcel IA，65:30:5己 烧/(己烧：i-Pr0H: CH30H = 90 : 5 : 5)/i-Pr0H，0 · 7mL/min)]测定，tr(major) = 66 · Imin，tr (minor) =60 · Omin0
实施例59: (2R，3S)_乙基1-(I-萘酰氨基)-5-氧代-3-苯基吡咯烷-2- 羧酸酯：白色固体，trans:cis = 6:1，两种异构体的产率71 % ; [a]〇23(c 0.9，CHCl3) = -15;? 匪R(400MHz，CDCI3)S8.48((1, J = 8.0Hz，lH)，8 ·00((!，J = 8.0Hz，lH)，7.90(d，J = 7.6Hz， 1H) ,7.79(d ,J = 6.8Hz 1H), 7.62-7.41 (m, 7H), 7.36-7.34(m, 1H) ,4.85(d ,J = 5.6Hz , 1H), 4.29- 4.18(m,2H) ,3.65-3.59(m,2H) ,3.03(dd,J=17.6,8.0Hz,lH) ,2.74(dd,J = 17.6, 6.8Hz，lH)，1.24(t，J = 7.2Hz，3H);13C NMR(mixture of both isomers，100MHz，CDCI3)S 172.6,171.1,168.3,141.5,133.9,132.1,130.7,130.5,129.4,128.7,128.6,128.0， 127.8.127.4.127.0. 126.4.125.5.125.2.124.8.124.7.67.5.62.2.62.0.40.9， 36.9.14.4；HRMS for C24H23N204[M+1!"Calculated:403.1658,Found:403.1643；95:5 e.r.由HPLC[Chiralcel 1厶，75:20:5己烷/(己烷：卜卩抑!1:013011 = 90:5:5)八^^0!1，0.711117 min)]测定，tr(major) = 107 · 2min，tr(minor) = 120 · 6min〇
实施例60: (2R，3S)-乙基3-(4-氯苯基)-5-氧代吡咯烷-2-羧酸酯： 黄色油；[a]D23(c 0.67 ,CH2CI2) =_66.6。；H NMR(400MHz，CDCI3)S = 1.27(t，J = 7.2Hz，3H)， 2.49(dd，J=17.6Hz，6.8Hz，lH)，2.86(dd，J=17.2,9.6Hz，lH)，3.68-3.7