, 3. 32-3. 36 (m,1H),3. 18-3. 22 (m,1H),2. 96-3. 10 (m,4H)
[0307] 實施例33
[0308] 4_ (4-氣-3-(5-甲基-1,2, 3,4, 5,6_ 六氛P比略并[3,4_c] P比略-2-幾基)芐基) 酞嗪-1(2H)_酮
[0309]
[0310] IH NMR (400MHz, DMS0-d6) : δ 12. 59 (s, 1H) , 8. 26 (dd, J = 8Hz&0. 8Hz, 1H), 7. 96 (d,J = 7. 6Hz,1H),7. 90-7. 86 (m,1H),7. 84-7. 80 (m,1H),7. 43-7. 40 (m,2H), 7. 25-7. 21 (m,1H),4. 32 (s,2H),4. 19 (s,2H),3. 58 (s,2H),3. 43 (s,2H),2. 42 (s,3H) ·
[0311] 實施例34
[0312] 4_ (3-((3aR,8bR)-十氫吡略并[3,4_a]吡略嘆-2-幾基)-4-氟芐基)釀 嗪-1(2H)-酮
[0313]
[0314] IH NMR(400MHz,DMS0-d6) : δ 1〇· 5-10. 2(d,1H),8· 44-8. 46(m,1H),7· 71-7. 77(m, 3H),7.41-7.38(m,lH),7.24(d,J = 2.4Hz,lH),7.02-6.99 (m,lH),4.24(s,2H), 3. 89-0. 88 (m, 15H).
[0315] 實施例35
[0316] 4-(4-氟-3-(2-甲基-2,4,5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)芐基)酞 嗪-1(2H)-酮
[0317]
[0318] IH NMR(400MHz,CDC13) : δ 10. 〇2(s,1H),8. 44-8. 46(m,1H),7. 69-7. 79(m,3H), 7· 29-7. 40 (m,2H),7· 04-7. 17 (m,2H),4· 73-4. 77 (brd,2H),4· 37-4. 39 (brd,2H),4· 28 (s, 2H), 3. 89-3. 90 (brd, 2H).
[0319] 實施例36
[0320] 4-(4-氟-3-(I-甲基-2,4, 5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)芐基)酞 嗪-1(2H)-酮
[0321]
[0322] IH NMR(400MHz,CDC13) : δ 9. 98(s,1H),8. 44-8. 47 (m,1H),7· 70-7. 80 (m, 3H),7· 31-7. 40 (m,2H),7· 06-7. 30 (m,2H),4· 72-4. 78 (brd,2H),4· 37-4. 44 (brd,2H), 4· 28-4. 29 (brd,2H),3· 73-3. 85 (brd,3H) ·
[0323] 實施例37
[0324] 2-((5-(2-氟-5-((4-氧代-3,4-二氫酞嗪-I-基)甲基)芐基)六氫吡咯并[3, 4-c]吡咯-2 (IH)-基)甲基)-6-甲氧基吡啶-1-氧化物
[0325]
[0326] IH NMR(400MHz,DMS0-d6) : δ 12. 70 (s,1H),8· 26 (d,J = 8. 8Hz,1H), 8· 83-8. 91 (m,3H),7· 67-7. 70 (m,1H),7· 41-7. 45 (m,1H),7· 28-7. 30 (m,1H),7· 16-7. 23 (m, 1H),6· 82 (d,J = 8Hz,1H),4· 40-4. 41 (brd,2H),4· 31 (s,2H),3· 82 (s,3H),3· 70-3. 73 (brd, 1H),3. 37-3. 47 (m,3H),3. 12-3. 25 (m,3H),2. 99-3. 02 (brd,1H) ·
[0327] 實施例38
[0328] 4_ (3- (5-(二氟甲基)八氫P比略并[3,4_c] P比略-2-幾基)-4-氟芐基)釀 嗪-1(2H)-酮
[0329]
[0330] IH NMR(400MHz,CDC13) : δ 10. 25(s,1H),8. 45-8. 47(m,1H),8· 21-8. 24(m,1H), 7· 71-7. 79 (m,3H),7· 30-7. 32 (m,1H),7· 26-7. 29 (m,1H),7· 01-7. 05 (m,1H),4· 27 (s,2H), 3· 87-3. 93 (m,1H),3· 73-3. 82 (m,1H),3· 56-3. 70 (m,1H),3· 46-3. 50 (m,1H),3· 30-3. 34 (m, 1H),3· 18-3. 23 (m,1H),2· 92-2. 95 (m,1H) ·
[0331] 實施例39
[0332] 4- (4-氟-3- ((3aR,6aS) -5-氧代八氫環(huán)戊并[c]吡咯-2-羰基)芐基)酞 嗪-1(2H)-酮
[0333]
[0334] IH NMR(400MHz,CDC13) : δ 10. 63(s,1H),8. 47-8. 49(m,1H),7· 72-7. 81 (m,3H), 7· 37-7. 39 (m,1H),7· 30-7. 33 (m,1H),7· 02-7. 04 (brt,1H),4· 30 (s,2H),3· 95-4. 00 (m,1H), 3· 55-3. 65 (m,2H),3· 18-3. 22 (m,1H),2· 94-3. 10 (m,2H),2· 44-2. 61 (m,2H),2· 22-2. 28 (m, 1H),2· 08-2. 18(m,1H).
[0335] 實施例40
[0336] I乙基和2乙基4-(3-(2,4, 5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)-4-氟芐基) 酞嗪-I (2H)-酮的混合物
[0337]
[0338] IH NMR(400MHz,DMS0-d6) : δ 12. 60(s,1H),8. 25(t,1H),7. 99(dd,J = 7· 6HzMHz,1H),7· 91-7. 87 (m. 1H),7· 85-7. 81 (m,1H),7· 61-7. 42 (m,3H),7· 28-7. 23 (m, 1Η),5· 31 (s,1Η),4· 55(d,1Η),4· 52-4. 43 (d,2H),4· 34(s,2H),4· 28-4. 20 (t,2H), 4· 14-4. 08 (m,2Η),3· 39-3. 35 (m,2Η),I. 67-1. 10 (m,6Η) ·
[0339] 實施例41
[0340] 4-(3-(2-乙基-2,4, 5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)-4-氟芐基)酞 嗪-1(2H)-酮
[0341]
[0342] IH NMR(400MHz,DMS0-d6) : δ 12. 59(s,1H),8. 26(d,J = 8Hz,1H),7. 98(d,J = 7. 6Hz,1H),7· 88(d,J = 8Hz,1H),7· 84(d,J = 7. 6Hz,1H),7· 61(s,1H),7· 46(d,J = 5. 6Hz, 2H),5. 25 (m,1H),4. 55 (s,2H),4. 33 (s,2H),4. 26 (d,2H),4. 10 (q,2H),I. 36-1. 32 (m,3H) ·
[0343] 實施例42
[0344] 4-(3-(1-乙基-1,4, 5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)-4-氟芐基)酞 嗪-1(2H)-酮
[0345]
[0346] IH NMR (400MHz,DMS0-d6) : δ 10. 37-10. 34(d,2H),8· 47-8. 45 (dd,1H), 7· 82-7. 22 (m,3H),7· 41-7. 33 (m,2H),7· 20 (s,1H),7· 13-6. 99 (m,1H),4· 82 (s,1H),4· 72 (s, 1Η),4· 46 (s,1Η),4· 37 (s,1Η),4· 37-4. 31 (d,2Η),4· 15 (q,2Η),I. 48 (t,2Η),I. 37 (t,1Η) ·
[0347] 實施例43
[0348] 4-(4-氟-3-(I-異丙基-I,4, 5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)芐基)酞 嗪-1(2H)-酮
[0349]
[0350] lHMMR(400MHz,DMS0-d6):Sl2.56(s,lH),8.24(d,J = 7.6Hz,lH),7.95(t, 1H),7· 87 (t,1H),7· 81 (t,1H),7· 46-7. 42 (m,2H),7· 27-7. 22 (m,1H),7· 15 (s,1H),4· 74 (s, 1H),4· 48(s,1H),4· 45(m,1H),4· 32(s,2H),4· 30-4. 26(m,1H),4· 16(s,1H),I. 37(d,3H), I. 23(t,3H).
[0351] 實施例44
[0352] (I異丙基和2異丙基)4-(4-氟-3-(1,4,5,6-四氫吡咯并[3,4-(:]吡唑-5-羰 基)芐基)酞嗪-I (2H)-酮的混合物
[0353]
[0354] IH NMR(400MHz,DMS0-d6) : δ 12. 58(s,1H),8. 26(d,J = 7. 6Hz,1H),7. 98(d,J =8Hz,1H),7· 91-7. 81 (m,2H),7· 48-7. 42 (m,2H),7· 29-7. 23 (m,1H),7· 17 (s,1H),4· 55 (s, 1H),4. 49-4. 44 (m,1H),4. 33 (s,2H),4. 29 (s,1H),4. 24 (s,1H),I. 40 (dd,5H),I. 25 (t,1H) ·
[0355] 實施例45
[0356] 4-(4-氟-3-(2-異丙基-2,4, 5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)芐基)酞 嗪-1(2H)-酮
[0357]
[0358] lHMMR(400MHz,DMS0-d6):Sl2.57(s,lH),8.26(d,J = 7.6Hz&1.2Hz,lH), 7. 98 (t,1H),7. 91-7. 87 (m,1H),7. 85-7. 81 (m,1H),7. 64-7. 50 (d,1H),7. 46-7. 42 (m,2H), 7. 27(t,1H),4. 55(s,2H),4. 49-4. 46(m,1H),4. 33(s,2H),4. 29(s,1H),4. 24(s,1H), I. 40-1. 38(dd,6H).
[0359] 實施例46
[0360] 4_ (3- ((3aR,6aS) -5, 5_二氣八氛環(huán)戊并[c]吡略-2-幾基)-4-氣芐基)釀 嗪-1(2H)-酮
[0361]
[0362] IH NMR(400MHz,: ? 1〇· 07 (s,1Η),8· 45-8. 47 (m,1Η),7· 70-7. 79(m,3H), 7· 35-7. 37 (m,1Η),7· 24-7. 31 (m,1Η),7· 01-7. 05 (brt,1Η),4· 27 (s,2Η),3· 82-3. 87 (m,1Η), 3· 65-3. 70 (m,1Η),3· 51-3. 56 (m,1Η),3· 18-3. 22 (m,1Η),2· 80-2. 94 (m,2Η),2· 26-2. 45 (m, 2Η),I. 87-2. 08(m,2H).
[0363] 實施例47
[0364] 4-(4-氟-3-(5-(2-甲氧基乙基)八氫吡咯并[3,4-c]吡咯-2-羰基)芐基)酞 嗪-1(2H)-酮
[0365]
[0366] IH NMR(400MHz,CDC13) : δ 10. 25(s,1H),8. 44-8. 47(m,1H),7· 71-7. 79(m,3H), 7· 34-7. 36 (m,1H),7· 26-7. 30 (m,1H),6· 99-7. 04 (brt,1H),4· 27 (s,2H),3· 64-3. 79 (m,2H), 3· 50-3. 53 (m,2H),3· 42-3. 47 (m,1H),3· 36 (s,3H),3· 16-3. 18 (brd,1H),2· 80-2. 97 (m,2H), 2· 64-2. 68 (m,2H),2· 41-2. 42 (brd,1H) ·
[0367] 實施例48
[0368] N- ((3aR,6aS) -2- (2-氟-5- ((4-氧代-3,4-二氫酞嗪-I-基)甲基)芐基)八氫 環(huán)戊并[c]吡咯-5-基)環(huán)丙烷甲酰胺
[0369]
[0370] IH NMR(400MHz,CDC13) : δ 10. 38(s,1H),8. 44-8. 46(m,1H),7. 72-7. 78(m,3H), 7· 42-7. 44 (m,1H),7· 26-7. 29 (m,1H),6· 98-7. 03 (brt,1H),5· 57 (brd,1H),4· 40-4. 42 (m, 1H),4· 27 (s,2H),3· 79-3. 85 (m,1H),3· 48-3. 60 (m,2H),3· 06-3. 10 (m,1H),2· 78-2. 85 (m, 2H),I. 90-2. 00 (m,1H),I. 70-1. 88 (m,1H),I. 00-1. 03 (m,2H),0· 83-0. 90 (m,1H), 0· 73-0. 75 (m,2H)
[0371] 實施例50
[0372] 4-(4-氟-3-(1-甲基-2,4, 5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)芐基)酞 嗪-1(2H)-酮氫溴酸鹽
[0373]
[0374] IH NMR(400MHz,DMS0-d6) : δ 12. 59(d,J = 3. 6Hz,1H),8. 26(d,J = 7. 6Hz, 1H),8· 005-7· 92(m,1H),7· 911-7. 87(m,1H),7· 85-7. 81 (m,1H),7· 48-7. 43(m,2H), 7. 30-7. 25 (m,1H),7· 15(brs,1H),4· 69(s,1H),4· 53(s,1H),4· 42(s,1H),4· 34(s,2H), 4. 21 (s,1H),3. 78-3. 66 (brd,3H) ·
[0375] 實施例51
[0376] 4-(4-氟-3-(I-甲基-2,4, 5,6-四氫吡咯并[3,4-c]吡唑-5-羰基)芐基)酞 嗪-1(2H)_酮鹽酸鹽
[0377]
[0378] IH NMR (400MHz,DMS0-d6) : δ 12. 59-12. 59 (d,J = 3·6Ηζ,1H),8.26 (d,J = 7·6Ηζ, 1H),7. 98 (t,J = 8Hz,1H),7. 89 (t,J = 3. 4Hz,1H),7. 83 (t,J = 7. 4Hz,1H),
[0379] 7. 43-7. 48 (m,2H),7. 26-7. 28 (m,1H),7. 15-7. 27 (brd,1H),4. 53-4. 69 (brd,2H), 4. 34 (s,2H),4. 21-4. 42 (brd,2H),3. 66-3. 78 (brd,3H) ·
[0380] 實施例52
[0381] 4-(4-氟-3-(1-甲基-1,4,5,6-四氫吡咯并[3,4-(:]吡唑-5-羰基)芐基)酞 嗪-I (2H)-酮硫酸鹽
[0382]
[0383] IH NMR(400MHz DMS〇-d6) : δ 12. 59-12. 58 (d, J = 3. 2Hz,1H),8. 26(d, J = 8Hz, 1H),7· 97(m,1H),7· 89(m,1H),7· 84(m,1H),7· 48-7. 43(m,2H),7· 15(s,1H),4· 53(s,1H), 4. 41 (s,1H),4. 34 (s,2H),4. 21 (5,1H),3. 78 (s,3H),3. 73 (m,1H) ·
[0384] 實施例53