(4-氣苯基)-2-氧代-1,2-二氨化晚-3-甲酯胺的制備
[04%]
[0427] 1h NMR(400MHz,CDCl3)Sl2.02(s,1H),8.76-8.74(m,lH),8.56(s,2H),7.99-7.95 (m,lH),7.89(d,J = 5.6Hz,lH),7.84(d,J = 3.2Hz,lH),7.65-7.63(m,lH),7.57(d,J = 6.0Hz,2H),7.42-7.33(m,4H),7.29-7.25(m,lH),7.13-7.09(m,lH),6.96(d,J=2.細z, lH),6.63(t,J = 7.2Hz,lH),5.79-5.78(m,lH)
[0428] MS:536[M+扣+
[0429] 實施例58)4-乙氧基-N-(4-((5-(2-乙氧基化晚-4-基)化咯并[l,2-b]化嗦-4- 基)-氧)-3-氣苯基)-1-(4-氣苯基)-2-氧代-1,2-二氨化晚-3-甲酯胺的制備
[0430]
[0431] 1h NMR(400MHz,CDCl3)Sll.64(s,lH),8.07(d,J = 5.6Hz,lH),7.94(dd,J=12.^P 2.4Hz,lH),7.86(d,J = 5.2Hz,lH),7.80(d,J = 2.Wz,lH),7.50(d,J = 8.0Hz,lH),7.37- 7.33(m,2H),7.29-7.26(m,lH),7.25-7.21(m,2H),7.18(dd,J = 5.2和l.細z,lH),7.07(t,J =8.細z,lH),6.98(d,J=1.2Hz,lH),6.93(d,J = 3.2Hz,lH),6.35(d,J = 8.0Hz,lH),5.75 (dd,J = 5.6和1.2Hz,lH),4.35(q,J = 7.2Hz,2H),4.33(q,J = 7.2Hz,2H),1.58(t,J = 7.2Hz,3H),1.38(t,J = 7.2Hz,3H)
[0432] MS:624[M+扣+
[0433] 實施例59)4-乙氧基-N-(3-氣-4-((5-(2-甲氧基化晚-4-基川比咯并[1,2-6]化嗦- 4-基)氧)苯基)-1 -(4-氣苯基)-2-氧代-1,2-二氨R比晚-3-甲酯胺的制備
[0434]
[0435] 1h NMR(400MHz,CDCl3)Sll.64(s,lH),8.10(d,J = 5.2Hz,lH),7.94(dd,J = 2.巧口 12.4Hz,lH),7.86(d,J = 5.2Hz,lH),7.81(d,J = 3.2Hz,lH),7.51(d,J = 7.細z,lH),7.38- 7.:M(m,2H),7.29-7.21(m,2H),7.19(dd,J = 1.2和5.細z,lH),7.07(t,J = 8.8Hz,lH),7.02 (m,lH),6.93(d,J = 3.2Hz,lH),6.36(d,J = 7.細z,lH),5.75(d,J = 5.2Hz,lH),4.36(q,J = 7.2Hz,lH),3.93(s,3H),1.58(t,J = 7.2Hz,3H)
[0436] MS:610[M+扣 +
[0437] 實施例60)N-(3-氣-4-((5-(化晚-4-基川比咯并[1,2-6]化嗦-4-基)氧)苯基)-4- 乙氧基-2-氧代-1-苯基-1,2-二氨化晚-3-甲酯胺的制備
[0438]
[0439] 1h NMR(400MHz,CDCl3)Sll.75(s,lH),8.53(d,J = 6.0Hz,2H),8.00-7.95(m,lH), 7.88(d,J = 5.細z,lH),7.83(d,J = 2.8Hz,lH),7.58-7.54(m,3H),7.37-7.:M(m,3H),7.30- 7.22(m,2H) ,7.08-7.04(m,lH),6.95(d,J = 2.細z,lH),6.40(d,J = 8.0Hz,IH) ,5.79-5.77 (m,lH),4.10(s,3H)
[0440] MS:566[M+扣 +
[0441 ] 實施例61)N-(4-((5-(2,6-二甲基化晚-4-基川比咯并[l,2-b]化嗦-4-基)氧)-3- 氣苯基)-4-乙氧基-1-(4-氣苯基)-2-氧代-l,2-二氨R比晚-3-甲酯胺的制備
[0442]
[0443] 1h NMR(400MHz,CDCl3)δll.67(s,lH),7.98(dd,J=12.8和2.4Hz,lH),7.88(d,J = 5.2Hz,lH),7.81(d,J = 2.4Hz,lH),7.52(d,J = 7.6Hz,lH),7.38-7.:M(m,2H),7.28-7.22 (m,甜),7.06(t,J = 8.8Hz,lH),6.93(d,J = 2.8Hz,lH),6.38(d,J = 8.0Hz,lH),5.78(d,J = 5.2Hz,lH),4.36(q,J = 7.2Hz,2H),2.53(s,細),1.59(t,J = 7.2Hz,3H)
[0444] MS:608[M+扣 +
[0445] 實施例62)N-(4-((5-(2-(l-^基乙基)化晚-4-基)化咯并[l,2-b]化嗦-4-基) 氧)-3-氣苯基)-4-乙氧基-1-( 4-氣苯基)-2-氧代-1,2-二氨R比晚-3-甲酯胺的制備
[0446]
[0447] 1h NMR(400MHz,CDCl3)Sll.67(s,lH),8.46(d,J = 5.2Hz,lH),7.98-7.95(m,lH), 7.89(d,J = 5.細z,lH),7.83(d,J = 2.細z,lH),7.57(s,lH),7.51(d,J = 7.細z,lH),7.48- 7.47(m,lH) ,7.38-7. :M(m,2H) ,7.30-7.22(m,3H) ,7.08-7.03(m,lH),6.97(d,J = 2.細z, lH),6.37(d,J = 8.0Hz,lH),5.78(d,J = 5.2Hz,lH),4.87(q,J = 6.4Hz,lH),4.37(q,J = 6.8Hz,2H),1.59(t,J = 6.細z,3H),1.44(d,J = 4.8Hz,3H)
[044引 MS:624[M+扣 +
[0449]實施例63)N-(4-((5-(3-((二甲氨基)甲基)苯基)郵咯并[l,2-b]惦嗦-4-基)氧)- 3-氣苯基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0450]
[0451 ] 1h NMR(400MHz,CDCl3)S9.94(s,lH),8.10(s,1H),7.82-7.80(m,2H),7.73-7.70 (m,lH),7.60(s,lH),7.53(d,J = 6.細z,lH),7.46-7.42(m,2H),7.33-7.29(m,lH),7.20- 7.17(m,2H),7.14-7.04(m,3H),6.91(d,J = 2.8Hz,lH),5.65(d,J = 5.6Hz,lH),3.42(s, 2H),2.18(s,6H),1.82-1.79(m,2H),1.69-1.60(m,2H)
[0452] MS:624[M+扣+
[0453] 實施例64)N-(4-((5-(3-氨基苯基川比咯并[l,2-b]化嗦-4-基)氧)-3-氣苯基)-N- (4-氣苯基)環丙烷-1,1 -二甲酯胺的制備
[0454]
[0455] 1h NMR(400MHz,CDCl3)S9.92(s,lH),8.24(s,lH),7.81-7.79(m,2H),7.73-7.70 (m,IH),7.49-7.42(m,2H),7.18-7.15(m,lH),7.13-7.01(m,6H),6.88(d,J=2.細z,lH), 6.59-6.57(m,IH),5.66(d,J = 5.2Hz,lH),l.79-1.76(m,2H),1.69-1.58(m,2H)
[0456] MS:540[M+扣+
[0457] 實施例65)N-(4-((5-(3-乙酷氨基苯基)化咯并[l,2-b]化嗦-4-基)氧)-3-氣苯 基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[045引
[0459] 1h 醒R(400MHz,CDCl3)S9.94(s,lH),8.43(s,lH),7.82-7.78(m,2H),7.70-7.67 (m,lH),7.61(s,lH),7.47-7.41(m,3H),7.39-7.37(m,lH),7.29-7.24(m,2H),7.14-7.12 (m,lH),7.09-7.01(m,3H),6.86(d,J = 2.Wz,lH),5.68(d,J = 5.2Hz,lH),2.15(s,3H), 1.76-1.73(m,2H),1.69-1.57(m,2H)
[0460] MS:582[M+扣 +
[0461 ] 實施例66)N-(4-((5-(3-氨基-4-氣苯基川比咯并[l,2-b]化嗦-4-基)氧)-3-氣苯 基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0462]
[0463] 1h NMR(400MHz,CDCl3)S9.95(s,lH),8.18(s,lH),7.81-7.77(m,2H),7.74-7.70 (m,lH),7.45-7.42(m,2H),7.19-7.16(m,lH),7.12-7.00(m,4H),6.94(d,J=8.4Hz,2H), 6.83(d,J = 2.細z,lH),5.66(d,J = 5.2Hz,lH),3.75(s,2H),1.79-1.75(m,2H),1.65-1.58 (m,2H)
[0464] MS:558[M+扣+
[0465] 實施例67)N-(4-((5-(3-氨基-5-氯基苯基)郵咯并[l,2-b]惦嗦-4-基)氧)-3-氣 苯基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0466]
[0467] 1h NMR(400MHz,CDCl3)Sl0.03(s,lH),8.36(s,lH),7.87-7.80(m,2H),7.68-7.63 (m,3H),7.55-7.54(m,lH),7.48-7.43(m,3H),7.31(s,lH),7.19(s,lH),7.08-7.03(m,2H), 6.86-6.81 (m,2H),5.75(d,J = 5.細z,lH),1.78-1.69(m,2H),1.65-1.55(m,2H)
[0468] MS:565[M+扣+
[0469] 實施例68)N-(4-((5-(3-((二甲氨基)甲基)苯基川比咯并[1,2-M達嗦-4-基]氧)- 3-氣苯基)-1-( 4-氣苯基)-6-甲基-2-氧代-1,2-二氨R比晚-3-甲酯胺的制備
[0470]
[0471] 1h 醒尺(4001化,〔0(:13)811.89(3,把),8.63((1,1 = 7.6化,把),7.92((1(1,1=12.4和 2.4Hz,lH),7.81(d,J = 5.2Hz,lH),7.79(d,J = 2.8Hz,lH),7.61(s,lH),7.53(d,J = 7.細z, lH),7.33-7.29(m,3H),7.26-7.19(m,4H),7.08(t,J = 8.4Hz,lH),6.90(d,J = 2.細z,lH), 6.51(d,J = 7.6Hz,lH),5.67(dd,J = 5.2Hz,lH),3.45(s,2H),2.18(s,細),2.13(s,3H)
[0472] MS:589[M+扣+
[0473] 實施例69)N-(4-((5-(3-氨基甲酯苯基)化咯并[l,2-b]化嗦-4-基)氧)-3-氣苯 基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0474]
[04巧]1h NMR(400MHz,CDCl3)Sl0.09(s,lH),8.75(s,lH),7.83-7.81(m,2H),7.78-7.66 (m,4H),7.46-7.39(m,3H),7.18-7.16(m,lH),7.07-6.99(m,3H),6.89(d,J=2.細z,lH), 6.24(s,lH),5.79(s,lH),5.68(d,J=5.2Hz,lH),1.73-1.70(m,2H),1.61-1.58(m,2H)
[0476] MS:568[M+扣+
[0477] 實施例70)N-(4-((5-(3-氨基甲基苯基)化咯并[l,2-b]化嗦-4-基)氧)-3-氣苯 基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備 [0478]
[04巧]1h NMR(400MHz,CDCl3)S9.88(s,lH),8.70(s,lH),7.79-7.77(m,2H),7.58-7.43 (m,5H),7.31-7.27(m,lH),7.20-7.18(m,lH),7.11-7.09(m,lH),7.05-6.94(m,3H),6.84 (d J = 2.8Hz,lH),5.72(d,J = 5.2Hz,lH),3.93(s,2H),3.13(q J = 7.2Hz,2H),1.39-1.32 (m,4H)
[0480] MS:554[M+扣+
[0481 ] 實施例71)N-(4-((5-(3-^基甲基苯基)化咯并[l,2-b]化嗦-4-基)氧)-3-氣苯 基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0482]
[0483] 1h NMR(400MHz,CDCl3)S9.90(s,lH),8.:M(s,lH),7.80-7.79(m,2H),7.68-7.63 (m,2H),7.56(d,J = 7.Wz,lH),7.45-7.40(m,2H),7.33(t,J = 7.6Hz,lH),7.24-7.12(m, 2H),7.08-7.01(m,3H),6.88(d,J = 2.細z,lH),5.67(d,J = 5.細z,lH),4.68(s,2H),1.74- 1.71(m,2H),1.61-1.52(m,2H)
[0484] MS:555[M+扣 +
[0485] 實施例72)N-(4-((5-(3-(甲氨基)苯基)化咯并[l,2-b]化嗦-4-基)氧)-3-氣苯 基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0486]
[0487] 1h NMR(400MHz,CDCl3)S9.90(s,lH),8.23(s,lH),7.80-7.79(m,2H),7.73-7.69 (m,lH),7.46-7.41(m,2H),7.19-7.15(m,2H),7.12-6.99(m,4H),6.95-6.94(m,lH),6.91 (d,J = 2.8Hz,lH),6.53-6.51(m,lH),5.63(d,J = 5.2Hz,lH),2.81(s,3H),1.78-1.75(m, 2H),1.60-1.57(m,2H)
[0488] MS:554[M+扣+
[0489] 實施例73)N-(4-((5-(3-(乙氨基)苯基)化咯并[l,2-b]化嗦-4-基)氧)-3-氣苯 基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0490]
[0491 ] 1h NMR(400MHz,CDCl3)S9.91(s,lH),8.23(s,1H),7.80-7.79(m,2H),7.73-7.69 (m,lH),7.45-7.41(m,2H),7.18-7.03(m,5H),7.00-6.97(m,lH),6.94-6.93(m,lH),6.90 (d,J = 2.8Hz,lH),6.52-6.50(m,lH),5.64-5.62(m,lH),3.13(q,J = 7.2Hz,2H),1.78-1.75 (m,2H),1.60-1.57(m,2H),1.21(t,J = 2.4,3H)
[0492] MS:568[M+扣+
[0493] 實施例74)N-(4-((5-(lH-嗎隙-6-基川比咯并[1,2-帥達嗦-4-基)氧)-3-氣苯基)- N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0494]
[04 巧]iHNMR(400MHz,CDCl3)S9.84(s,lH),8.28-8.23(m,2H),7.81-7.77(m,2H),7.68- 7.64(m,2H),7.60(d J = 8.0Hz,lH) ,7.44-7.39(m,3H),7.14(tJ = 2.細z,lH) ,7.07-6.99 (m,4H),6.92(d,J = 2.細z,lH),6.52-6.51(m,lH),5.60(d,J = 0.細z,lH),1.72-1.69(m, 2H)a.56-1.52(m,2H)
[0496] MS:564[M+扣+
[0497] 實施例75)N-(4-((5-(2-氯-5-((二甲氨基)甲基)苯基)化咯并[l,2-b]化嗦-4- 基)氧)-3-氣苯基)-N- (4-氣苯基)環丙烷-1,1 -二甲酯胺的制備
[0498]
[0499] 1h NMR(400MHz,CDCl3)δ9.98(s,lH),8.07(s,lH),7.84(d,J = 5.細z,lH),7.80(d, J = 2.8Hz,lH),7.73(dd,J = 2.4,12Hz,lH),7.51(t,lH),7.48(s,lH),7.42-7.46(m,2H), 7.19-7.21(m,2H),7.13(t,lH),7.04-7.09(m,2H),6.89(d,J = 2.8Hz,lH),5.69(dd,J = 0.8,5.2Hz,lH),3.38(s,2H),2.27(s,6H),1.89(t,2H),4.60(t,2H)
[0 如 0] MS:616[M+扣 +
[0501 ]實施例76)N-(4-( (5-(5-((二甲氨基)甲基)-2-氣苯基)化咯并[l,2-b]化嗦-4- 基)氧)-3-氣苯基)-N- (4-氣苯基)環丙烷-1,1 -二甲酯胺的制備
[ο如 2]
[Ο如引 1η 醒R(400MHz,CDCl3)Sl0.13(s,lH),8.64(s,lH),7.83(d,J = 5.6Hz,lH),7.80 (d,J = 2.8Hz,lH),7.71(dd,J = 2.4,12Hz,lH),7.42-7.45(m,2H),7.36(s,lH),7.26-7.29 (m,lH),7.19-7.22(m,lH),7.01-7.11(m,3H),6.95(dd,J=1.2,9.2Hz,lH),6.88(d,J = 2.細z,lH),5.70(d,J=5.2Hz lH),3.58(s,2H),2.33(s,細),1.74-1.77(m,2H),1.60-1.63 (m,2H)
[0 如 4] MS:600[M+扣 +
[0505]實施例77)N-(4-( (5-(3-((二甲氨基)甲基)-5-氣苯基)化咯并[l,2-b]化嗦-4- 基)氧)-3-氣苯基)-N- (4-氣苯基)環丙烷-1,1 -二甲酯胺的制備
[0如 6]
[0如7] 1h NMR(400MHz,CDCl3)Sl0.12(s,lH),8.71(s,lH),7.81-7.84(m,2H),7.68(dd,J =2,12Hz,lH),7.41(m,lH),7.41-7.48(m,3H),7.18(m,2H),7.00-7.10(m,3H),6.90-6.91 (m,lH),5.67(d,J = 5.2Hz,lH),3.58(s,2H),2.27(s,細),1.75(t,2H),1.63(t,2H)
[0 如引 MS:600[M+扣 +
[0509] 實施例78)N-(4-((5-(3-氨基-4-甲基)-5-氣苯基)化咯并[l,2-b]化嗦-4-基) 氧)-3-氣苯基)-N- (4-氣苯基)環丙烷-1,1 -二甲酯胺的制備
[0510]
[0511] 1h 醒R(400MHz,CDCl3)S9.95(s,lH),8.45(s,lH),7.79-7.68(m,3H),7.44-7.40 (m,2H),7.16-6.99(m,W),6.86(dJ = 2.Wz,lH),6.18-6.16(m,lH),5.63(dJ = 5.2Hz, IH),2.17(s,3H),1.78-1.71(m,2H),1.60-1.53(m,2H)
[0512] MS:554[M+扣+
[OSU] 實施例79)N-(4-((5-(3-氨基-2-甲基)-5-氣苯基)化咯并[l,2-b]化嗦-4-基) 氧)-3-氣苯基)-N- (4-氣苯基)環丙烷-1,1 -二甲酯胺的制備
[0514]
[0515] 1h NMR(400MHz,CDCl3)Sl0.37(s,lH),8.69(s,1H),7.79-7.78(m,2H),7.62-7.58 (m,2H),7.47-7.40(m,2H),7.12-7.10(m,lH),7.03-6.92(m,3H),6.83(d,J=7.細z,lH), 6.71(d,J = 2.4Hz,lH),6.62(d,J = 8.0Hz,lH),5.58(d,J = 5.2Hz,lH),2.09(s,3H),1.71- 1.68(m,2H),1.59-1.56(m,2H)
[0516] MS:554[M+扣+
[0517] 實施例80)N-(3-氣-4-((5-(3-((甲氨基)甲基巧基)郵咯并[1,2-6]惦嗦-4-基) 氧)苯基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[051 引
[0519] 1h NMR(400MHz,CDCl3)S9.91(s,lH),8.37(s,lH),7.83(d,J = 5.2Hz,lH),7.81(d, J = 2.8Hz,lH),7.68(dd,J = 2.4Hz 和 12.4Hz,1H) ,7.52-7.58(m,2H) ,7.40-7.47(m,2H), 7.32(t,lH),7.16-7.21(m,3H),7.07(q,3H),6.90(d,J = 2.4Hz,lH),5.70(d,J = 5.2Hz, IH),3.79(s,2H),2.37(s,3H),l.77-1.96(m,2H),1.69(s,lH),l.59-1.63(m,2H)
[0520] MS:568[M+扣+
[0521] 實施例81)N-(4-((5-(3-((乙氨基)甲基)苯基川比咯并[l,2-b]化嗦-4-基)氧)-3- 氣苯基)-N-(4-氣苯基)環丙烷-l,l-二甲酯胺的制備
[0522]
[0W;3] 1h NMR(400MHz,CDCl3)S9.95(s,lH),8.47(s,lH),7.82(d,J = 5.2Hz,lH),7.80(d, 1 = 2.8化,相),7.69((1(1^ = 2.4化和12.4化,相),7.60(3,巧),7.54-7.56(111,相),7.42- 7.47(m,2H),7.32(t,lH),7.24(s,lH),7.17-7.19(m,lH),7.02-7.10(m,3H),6.90(d,J= 2.8Hz,IH),5.67(d,J=5.2Hz,IH),3.85(s,2H),2.68(q,2H),1.75-1.78(m,2H),1.59-1.62 (m,2H),1.41(s,lH)
[0524] MS:582[M+扣 +
[052引實施例82)n-(4-((5-(3-氨基-4-甲氧基)-5-氣苯基川比咯并[l,2-b]化嗦-4-基) 氧)-3-氣苯基)-N- (4-氣苯基)環丙烷-1,1 -二甲酯胺的制備
[0526]
[0527] 1h NMR(400MHz,CDCl3)S9.93(s,lH),8.29(s,lH),7.78-7.77(m,2H),7.72-7.68 (m,2H) ,7.44-7.40(m,2H) ,7.16-6.99(m,6H),6.83(d,J = 2.細z,lH),6.78(d,J = 8.4Hz, IH),3.84(s,甜),1.76-1.73(m,2H),1.59-1.56(m,2H)
[052引 MS:570[M+扣 +
[0529] 實施例83)N-(4-((5-(5-氨基-2-氣)-5-氣苯基)郵咯并[l,2-b]化嗦-4-基)氧)- 3-氣苯基)-N-(4-氣苯基)環丙烷-1,1-二甲酯胺的制備
[0530]
[0531] 1h NMR(400MHz,Me0D)S7.86(d,J = 5.2Hz,lH),7.80(d,J = 2.4Hz,lH),7.75-7.71 (m,lH),7.56-7.52(m,2H),7.33-7.29(m,lH),7.19-7.15(m,lH),7.07-7.03(m,2H),6.88- 6.85(m,lH) ,6.83-6.80(m,2H) ,6.64-6.60(m,lH),5.69(d,J = 0.細z,lH)
[0532] MS:558[M+扣+
[0533] 實施例84)N-(4-((5-(3-(甲基氨基甲酯)苯基川比咯并[l,2-b]化嗦-4-基)氧)-3- 氣苯基)-N- (4-氣苯基)環丙烷-1,1 -二甲酯胺的制備
[0534]
[053引 1h NMR(400MHz,CDCl3)Sl0.15(s,lH),8.73(s,lH),7.83-7.80(m,2H),7.70-7.64 (m,5H),7.46-7.41(m,2