CN103242229B - 一种用于神经退行性疾病领域的pet显像剂thk523前体的合成方法 - Google Patents
一种用于神经退行性疾病领域的pet显像剂thk523前体的合成方法 Download PDFInfo
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- CN103242229B CN103242229B CN201310122627.XA CN201310122627A CN103242229B CN 103242229 B CN103242229 B CN 103242229B CN 201310122627 A CN201310122627 A CN 201310122627A CN 103242229 B CN103242229 B CN 103242229B
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- 0 *C1CC2C=CC(*(CCC3)CCC3[N+]([O-])=O)NC2CC1 Chemical compound *C1CC2C=CC(*(CCC3)CCC3[N+]([O-])=O)NC2CC1 0.000 description 1
Abstract
Description
化合物1 | 48%HBr | 温度 | 反应时间 | 产率 | 化合物2 |
3g | 20ml | 100℃ | 1h | 82% | 2.30g |
3g | 300ml | 150℃ | 12h | 83% | 2.40g |
3g | 600ml | 180℃ | 24h | 82% | 2.30g |
化合物1 | 三溴化硼 | 温度 | 反应时间 | 产率 | 化合物2 |
3g | 2.7g | -15℃ | 1h | 82% | 2.30g |
3g | 13.5g | 5℃ | 12h | 84% | 2.50g |
3g | 27g | 25℃ | 24h | 82% | 2.30g |
化合物2 | 官能化组分 | 温度 | 反应时间 | 产率 | 化合物3 |
2.35g | 2.7g TBDPSOCH2CH2Br | 50℃ | 1h | 85% | 4.20g |
2.35g | 2.5g TBSOCH2CH2Br | 85℃ | 12h | 84% | 4.15g |
2.35g | 2.2g MEMOCH2CH2Br | 120℃ | 24h | 85% | 4.20g |
化合物3 | 无水醋酸 | 硼氢化钠 | 温度 | 反应时间 | 产率 | 化合物4 |
铜 | ||||||
3g | 0.5g | 3g | 20℃ | 1h | 82% | 2.30g |
3g | 2.5g | 30g | 35℃ | 8h | 84% | 2.45g |
3g | 5g | 60g | 50℃ | 16h | 83% | 2.4g |
化合物3 | 二氯化锡 | 温度 | 反应时间 | 产率 | 化合物4 |
3g | 4.5g | 60℃ | 1h | 82% | 2.30g |
3g | 22.5g | 100℃ | 8h | 84% | 2.45g |
3g | 45g | 130℃ | 16h | 83% | 2.4g |
化合物5 | 酸溶液 | 温度 | 反应时间 | 产率 | 化合物6 |
1g | 盐酸 | 20℃ | 30min | 88% | 600mg |
1g | 氢溴酸 | 60℃ | 5h | 89% | 625mg |
1g | 醋酸 | 100℃ | 10h | 89% | 625mg |
化合物5 | 溶剂 | 温度 | 产率 | 化合物6 |
1g | NH3的醇溶液 | 20℃ | 88% | 600mg |
1g | NH3的醇溶液 | 60℃ | 89% | 625mg |
1g | NH3的醇溶液 | 100℃ | 89% | 625mg |
化合物5 | 氢化试剂 | 温度 | 反应时间 | 产率 | 化合物6 |
1g | 5%Pd/C0.5g | 0℃ | 1h | 88% | 600mg |
1g | Pd/BaSO43g | 20℃ | 5h | 89% | 630mg |
1g | 5%Pd(OH)2/C4g | 40℃ | 10h | 89% | 630mg |
Claims (9)
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CN201310122627.XA CN103242229B (zh) | 2013-04-10 | 2013-04-10 | 一种用于神经退行性疾病领域的pet显像剂thk523前体的合成方法 |
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CN201310122627.XA CN103242229B (zh) | 2013-04-10 | 2013-04-10 | 一种用于神经退行性疾病领域的pet显像剂thk523前体的合成方法 |
Publications (2)
Publication Number | Publication Date |
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CN103242229A CN103242229A (zh) | 2013-08-14 |
CN103242229B true CN103242229B (zh) | 2015-09-02 |
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CN (1) | CN103242229B (zh) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN103613589B (zh) * | 2013-11-29 | 2016-03-30 | 江苏华益科技有限公司 | 一种用于神经退行性疾病领域的新型pet显像剂前体及标准品的合成方法 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
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US8691187B2 (en) * | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
EP2411057B1 (en) * | 2009-03-23 | 2020-05-06 | Eli Lilly and Company | Imaging agents for detecting neurological disorders |
KR20140053811A (ko) * | 2010-10-29 | 2014-05-08 | 클리노 가부시끼가이샤 | 타우 이미징 프로브 |
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Address after: 215500 No. 18 Fu Yu Road, Changshou City hi tech Material Industrial Park, Jiangsu, Suzhou Applicant after: Jiangsu Huayi Science & Technology Co., Ltd. Applicant after: Huashan Hospital Affiliated to Fudan University Address before: 215500 No. 18 Fu Yu Road, Changshou City hi tech Material Industrial Park, Jiangsu, Suzhou Applicant before: Changshu Huayi Chemical Co., Ltd. Applicant before: Huashan Hospital Affiliated to Fudan University |
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