冯氏配体——近3年在活性天然产物和药物合成领域的应用研究
2023-10-30 · 系列介绍 · 百灵威授权转载
四川大学冯小明院士科研团队专注于新型手性催化剂的设计合成、不对称催化反应、手性药物和天然产物的高效高选择性合成研究，其中独具特色的手性双氮氧配体（简称“冯氏配体”）能高效高选择性地催化50多种不对称催化反应，被诺贝尔化学奖得主Noyori教授评价为“代表一类优势手性配体”。 冯氏配体主要优势如下：
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手性催化剂和配体
叶龙武教授科研成果 | 一类新型双齿噁唑啉配体
五大不对称合成方法，优选常用试剂大盘点
有机分子催化剂——产品总数400+，更有前沿科研成果供应！
- 广谱性强：可用作有机小分子催化剂，也可作为配体与多种金属形成配合物催化剂，均显示出优良的立体选择性；
- 结构可调：兼具刚性和柔性，可根据反应需求进行取代基修饰；
- 溶解性好，性质稳定：极性、非极性溶剂都可溶，对水和空气不敏感，常温即可反应。
表1 冯氏配体在活性天然产物和药物合成领域的应用研究
| 催化体系 | 合成产物 | 生物活性 |
|---|---|---|
| L-PrMe2/Ce(OTf)3 L-PrMe3/Ba(OTf)2 | 非达司他、瑞匹洛坦和沙立佐坦中间体[1] | 药物中间体 |
| L-PrmtBu2/Co(OTf)2 | (S)-verapamil、(S)-E2025、(S)-sporochnol A、(+)-glutechimide、 (−)-aphanorphine、(+)-epilaurene、(R)-aminoglutethimide中间体[2] | 药物或天然产物中间体 |
| L-PiMe5/Ni(OTf)2 L-PiMe5/Nd(OTf)3 | 尼群地平、尼莫地平和非洛地平[3] | 治疗心脑血管疾病 |
| L-PiEt2Me/Sc(OTf)3 | 三唑类抗真菌药艾沙康唑、艾氟康唑等药物中间体[4] | 抗菌 |
| L-PrMe2Ad/Zn(BF4) •6H2O | 手性4-恶唑烷酮类化合物[5] | 抗菌 |
| L-PiPr2/Sc(OTf)3 | 具有16、18或20元环的手性大环双内酯化合物[6] | 抗菌、抗癌 |
| L-RaPr3/Y(OTf)3 | 六氢吡咯并异喹啉类化合物[7] | 抗菌、抗癌、抗病毒 |
| L-PiEt2/Zn(BF4) •6H2O L-TQ-(S)-EPh/Pr(OTf)3 | 手性吡咯啉基和吡唑啉基螺环氧化吲哚类化合物[8,9] | 抗菌、抗癌、抗病毒 |
| L-Ra(OCH2Ad)2/Ni(OTf)2 | 三尖杉二萜优势骨架六氢芴基内酯[10] | 抗菌、抗癌、抗病毒 |
| L-PiMe2/Mg(OTf)2 | 天然产物(+)-minovincine[11] | 镇痛、抗菌、抗癌、抗病毒 |
| L-RaPr2/Al(OTf)3 | 具有抗癌活性的天然产物eupomatilones[12] | 抗炎、抗癌、抗病毒 |
| L-PiPr2/Ni(OTf)2/手性亚磷酰胺/[Ir(cod)Cl]2 L-PiPr2/Co(BF4)2•6H2O/手性亚磷酰胺/[Ir(cod)Cl]2 | 具有抗癌活性的天然产物Rocaglaol[13] | 抗炎、抗癌、抗病毒 |
百灵威独家供应四川大学冯小明院士开发的冯氏手性氮氧配体系列产品，还可提供多种金属盐和溶剂等配套产品，助力药物研发领域研究！
冯氏手性氮氧配体
| 品名 | CAS | 货号 |
|---|---|---|
| NO-Feng-PDMPPy, L-PrMe2, 99% NO-冯-PDMPPy | 1330533-36-2 | 1595284 |
| NO-Feng-PDEtMPPi, L-PiEt2Me, 95% NO-冯-PDEtMPPi | 1502814-74-5 | 2699019 |
| NO-Feng-PDiPPPi, L-PiPr2, 99% NO-冯-PDiPPPi | 1000051-40-0 | 1595285 |
| NO-Feng-PDEtPPi, L-PiEt2, 95% NO-冯-PDEtPPi | 1313215-46-1 | 2699018 |
| NO-Feng-PDMPPi, L-PiMe2, 95% NO-冯-PDMPPi | 1227411-35-9 | 2699017 |
| NO-Feng-PDiPPRa, L-RaPr2, 95% NO-冯-PDiPPRa | 1005495-74-8 | 1595287 |
金属盐
| 品名 | CAS | 货号 |
|---|---|---|
| Aluminum trifluoromethanesulfonate, 99% 三氟甲磺酸铝 | 74974-61-1 | 474717 |
| Barium trifluoromethanesulfonate, 98% 三氟甲磺酸钡 | 2794-60-7 | 409558 |
| Cerium(III) trifluoromethanesulfonate, 98% 三氟甲磺酸铈(III) | 76089-77-5 | 407448 |
| Cobalt(II) trifluoromethanesulfonate, 98% 三氟甲磺酸钴(II) | 58164-61-7 | 2772130 |
| Cobalt tetrafluoroborate hexahydrate, 99% 四氟硼酸钴六水合物 | 15684-35-2 | 290410 |
| Magnesium trifluoromethanesulfonate, 98% 三氟甲磺酸镁 | 60871-83-2 | 152796 |
| Neodymium(III) trifluoromethanesulfonate, 98% 三氟甲烷磺酸钕 | 34622-08-7 | 491468 |
| Nickel(II) trifluoromethanesulfonate, 96% 三氟甲磺酸镍(II) | 60871-84-3 | 810702 |
| Scandium(III) triflate, 98% 三氟甲磺酸钪 | 144026-79-9 | 302513 |
| Nickel(II) tetrafluoroborate hexahydrate, 99% 四氟硼酸镍(II)六水合物 | 15684-36-3 | 93-2841 |
| Yttrium(III) trifluoromethanesulfonate, 98% 三氟甲磺酸钇(III) | 52093-30-8 | 214543 |
| Zinc tetrafluoroborate hydrate, 98% 四氟硼酸锌水合物 | 13826-88-5 | 93-3010 |
溶剂
| 品名 | CAS | 货号 |
|---|---|---|
| Acetonitrile, 99.9%, SuperDry, water≤10 ppm, J&KSeal 乙腈 | 75-05-8 | 980779 |
| Dichloromethane, 99.9%, SuperDry, with molecular sieves, water≤30 ppm, J&KSeal 二氯甲烷 | 75-09-2 | 908525 |
| Ethyl acetate, 99.5%, SuperDry, J&KSeal 乙酸乙酯 | 141-78-6 | 954403 |
| Petroleum ether, SuperDry, boiling range 60 - 90 ℃, J&KSeal 石油醚 | 8032-32-4 | 985069 |
相关产品
有机分子催化剂手性催化剂和配体
参考文献
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- Zhang F, Ren B T, Zhou Y, et al. Enantioselective construction of cis-hydroindole scaffolds via an asymmetric inverse-electron-demand Diels–Alder reaction: application to the formal total synthesis of (+)-minovincine[J]. Chemical Science, 2022, 13(19): 5562-5567.
- Tan Z, Chen L, Li L, et al. Asymmetric Synthesis of α-Methylene-γ-butyrolactones via Tandem Allylboration/Lactonization: a Kinetic Resolution Process[J]. Angewandte Chemie, 2023: e202306146.
- Xu Y, Wang H, Yang Z, et al. Stereodivergent total synthesis of rocaglaol initiated by synergistic dual-metal-catalyzed asymmetric allylation of benzofuran-3(2H)-one[J]. Chem, 2022, 8(7): 2011-2022.
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冯氏手性氮氧配体——可高效实现50多种不对称催化反应叶龙武教授科研成果 | 一类新型双齿噁唑啉配体
五大不对称合成方法，优选常用试剂大盘点
有机分子催化剂——产品总数400+，更有前沿科研成果供应！
