CN104109235B - 一种具有氮原子支化中心的单一官能化聚乙二醇、制备方法及其生物相关物质 - Google Patents
一种具有氮原子支化中心的单一官能化聚乙二醇、制备方法及其生物相关物质 Download PDFInfo
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- CN104109235B CN104109235B CN201410238134.7A CN201410238134A CN104109235B CN 104109235 B CN104109235 B CN 104109235B CN 201410238134 A CN201410238134 A CN 201410238134A CN 104109235 B CN104109235 B CN 104109235B
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- -1 methylene, 1, 2-ethylene, 1, 3-propylene, 1, 2-propylene, butylene, pentylene, hexylene, heptylene, octylene, nonylene, decylene Chemical group 0.000 claims description 327
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 89
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 74
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- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 40
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 39
- 229910052740 iodine Inorganic materials 0.000 claims description 38
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 37
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- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 14
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- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 12
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- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 12
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- JGVWCANSWKRBCS-UHFFFAOYSA-N tetramethylrhodamine thiocyanate Chemical compound [Cl-].C=12C=CC(N(C)C)=CC2=[O+]C2=CC(N(C)C)=CC=C2C=1C1=CC=C(SC#N)C=C1C(O)=O JGVWCANSWKRBCS-UHFFFAOYSA-N 0.000 description 1
- MPLHNVLQVRSVEE-UHFFFAOYSA-N texas red Chemical compound [O-]S(=O)(=O)C1=CC(S(Cl)(=O)=O)=CC=C1C(C1=CC=2CCCN3CCCC(C=23)=C1O1)=C2C1=C(CCC1)C3=[N+]1CCCC3=C2 MPLHNVLQVRSVEE-UHFFFAOYSA-N 0.000 description 1
- 229940021747 therapeutic vaccine Drugs 0.000 description 1
- ACOJCCLIDPZYJC-UHFFFAOYSA-M thiazole orange Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1.C1=CC=C2C(C=C3N(C4=CC=CC=C4S3)C)=CC=[N+](C)C2=C1 ACOJCCLIDPZYJC-UHFFFAOYSA-M 0.000 description 1
- 150000003555 thioacetals Chemical class 0.000 description 1
- 125000005323 thioketone group Chemical group 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
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- NZVYCXVTEHPMHE-ZSUJOUNUSA-N thymalfasin Chemical compound CC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(N)=O)C(O)=O NZVYCXVTEHPMHE-ZSUJOUNUSA-N 0.000 description 1
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- IVZTVZJLMIHPEY-UHFFFAOYSA-N triphenyl(triphenylsilyloxy)silane Chemical compound C=1C=CC=CC=1[Si](C=1C=CC=CC=1)(C=1C=CC=CC=1)O[Si](C=1C=CC=CC=1)(C=1C=CC=CC=1)C1=CC=CC=C1 IVZTVZJLMIHPEY-UHFFFAOYSA-N 0.000 description 1
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- 229920001567 vinyl ester resin Polymers 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
Landscapes
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
编号 | R0 | R名称 | 中间体 | 聚乙二醇分子量Mn(Da) |
S1 | A1 | 琥珀酰亚胺丙酸酯 | H1-2 | 15,000=5,000×2+5,000 |
S2 | A2 | 对硝基苯丙酸酯 | H1-1 | 20,000=8,500×2+3,000 |
S3 | A3 | 1,3,5-三氯苯丙酸酯 | 7-1 | 20,000=1,500×2+17,000 |
S4 | A5 | 苯并三唑丙酸酯 | H1-4 | 30,000=10,000×2+10,000 |
S5 | A8 | 咪唑丙酸酯 | H1-5 | 30,000=7,500×2+15,000 |
S6 | A14 | 苯并三唑丙酸酯 | H1-3 | 40,000=(10,000+5000)+25,000 |
L1 | A1 | 琥珀酰亚胺丙酸酯 | H1-2 | 15,000 |
L2 | A2 | 对硝基苯丙酸酯 | H1-1 | 20,000 |
L3 | A5 | 苯并三唑丙酸酯 | H1-4 | 30,000 |
L4 | A11 | 苯并三唑丙酸酯 | H1-3 | 40,000 |
LA | / | / | / | / |
编号 | R | 分子量Mn(Da) | t1/2(h) |
S1 | A1 | 15,000=5,000×2+5,000 | 42.7 |
S2 | A2 | 20,000=8,500×2+3,000 | 63.6 |
S3 | A3 | 20,000=1,500×2+17,000 | 58.3 |
S4 | A5 | 30,000=10,000×2+10,000 | 85.4 |
S5 | A8 | 30,000=7,500×2+15,000 | 78.2 |
S6 | A13 | 40,000=(10,000+5000)+25,000 | 67.8 |
L1 | A1 | 15,000 | 10.3 |
L2 | A2 | 20,000 | 16.9 |
L3 | A5 | 30,000 | 21.5 |
L4 | A13 | 40,000 | 24,1 |
L01 | / | / | 3.1 |
编号 | R | R名称 | L4类型 |
S7 | A1 | 琥珀酰亚胺碳酸酯 | 氨基甲酸酯基 |
S8 | A6 | 琥珀酰亚胺乙酸酯 | 酰胺键 |
S9 | A6 | 琥珀酰亚胺丙酸酯 | 酰胺键 |
S10 | C10 | 碘乙酰胺 | -NHC(=O)CH2-S- |
S11 | B3 | 乙烯基砜 | -S(=O)2CH2CH2S- |
S12 | C2 | 巯基 | 二硫键 |
S13 | C4 | 叠氮 | 异恶唑 |
S14 | D5 | 丙醛 | 酰胺键 |
S15 | E1 | 马来酰亚胺 | 仲胺基 |
S16 | G1 | 环炔基 | 三氮唑 |
L5 | A6 | 琥珀酰亚胺丙酸酯 | 酰胺键 |
L02 | A6 | 琥珀酰亚胺丙酸酯 | 仲胺基 |
Claims (57)
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