突破C-H官能化瓶颈：DMIX-高价碘试剂全新登场
2026-06-22 · 推荐产品 · 百灵威授权转载
【研究背景】
在现代有机合成中，通过C-H键直接官能化来构建复杂分子，是提高合成效率的革命性策略。当前主流手段包括：
- 过渡金属催化C-H活化：通过钯、铑、钌等金属催化剂实现选择性转化，常需导向基辅助定位，且金属残留问题在药物合成中尤为敏感。
- 锍盐介导的C-H官能化（如噻蒽锍盐）：通过形成锍盐中间体实现位点选择性官能化，但往往步骤较长。
- 高价碘（二芳基碘鎓盐）策略：兼具亲电性与离去能力，可在无金属条件下与多种亲核试剂偶联。但两大瓶颈——底物局限（仅限富电子芳烃）和芳基迁移选择性差——严重限制其应用。
【产品优势】
DMIX (3,5-二甲基-4-异噁唑基) -高价碘试剂可一步破解上述难题[1]：
- 不迁移基团：DMIX充当稳定“虚拟配体”，迁移能垒极高（计算表明比TMP更难转移），确保另一芳基高选择性迁移，避免异构体副产物。
- 底物普适广：同时兼容富电子与缺电子芳烃（含硝基、氰基、酯基等），突破传统局限。
- 条件温和：室温、无过渡金属、无需预官能化，操作简便，绿色环保。
- 试剂稳定：DMIX无芳香C-H键，避免自身聚合，易于储存。
【应用案例】
基于上述优势，DMIX高价碘试剂已在多个前沿领域展现应用潜力：
- 药物后期多样化修饰：对吉非罗齐、醚菊酯、美他沙酮、尼美舒利等药物直接C-H官能化，构建C-O/C-N/C-S键，加速SAR研究。
- 二芳基醚合成：两步无金属法从简单芳烃制备，收率高达95%。
- 区域选择性硝化：以NaNO₂为硝源，单一异构体收率高达98%，适用于氯苯等挑战底物。
- α-芳基氨基酸与硫醚构建：与丙二酸酯衍生物或黄原酸盐偶联，无金属条件下高效构筑C-C及C-S键。
- 大环分子精准编辑：实现杯[4]芳烃选择性单官能化，拓展材料化学应用。
百灵威稳定供应系列DMIX-高价碘试剂，助您快速实现复杂分子C-H官能化。
产品清单
| 品名 | CAS | 货号 |
|---|---|---|
| Hypoiodous acid, I-(3,5-dimethyl-4-isoxazolyl)-I-hydroxy-, (4-methylphenyl)sulfonyl ester, 98% 4-甲基苯磺酸(3,5-二甲基异噁唑-4-基)(羟基)碘酯 | 2776240-77-6 | 9455649 |
| Iodine, bis(acetato-κO)(3,5-dimethyl-4-isoxazolyl), 98% 二乙酰氧基(3,5-二甲基异噁唑-4-基)碘 | 2776240-78-7 | 9724127 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(2,4,6-trimethoxyphenyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(2,4,6-三甲氧基苯基)碘鎓对甲苯磺酸盐 | 2776240-80-1 | 9726725 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(4-ethylphenyl)-, 4-methylbenzenesulfonate(1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(4-乙基苯基)碘鎓对甲苯磺酸盐 | 2776240-82-3 | 9726726 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(4-pentylphenyl)-, 4-methylbenzenesulfonate(1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(4-戊基苯基)碘鎓对甲苯磺酸盐 | 2776240-84-5 | 9726727 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(4-phenoxyphenyl)-, 4-methylbenzenesulfonate(1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(4-苯氧基苯基)碘鎓对甲苯磺酸盐 | 2776240-87-8 | 9726728 |
| Iodonium, [4-(3-bromopropyl)phenyl](3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate(1:1) (ACI), 98% [4-(3-溴丙基)苯基](3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776240-86-7 | 9726729 |
| Hypoiodous acid, I-(3,5-dimethyl-4-isoxazolyl)-I-(4-methoxyphenyl)-, (4-methylphenyl)sulfonyl ester(ACI), 98% (3,5-二甲基异噁唑-4-基)(4-甲氧基苯基)碘鎓对甲苯磺酸盐 | 2971810-35-0 | 9726730 |
| Iodonium, (4-cyclopropylphenyl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate(1:1) (ACI), 98% (4-环丙基苯基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 3087723-85-8 | 9726731 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)[4-(2-propen-1-yloxy)phenyl]-, 4-methylbenzenesulfonate(1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)[4-(烯丙氧基)苯基]碘鎓对甲苯磺酸盐 | 2776240-89-0 | 9726732 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(2,4-dimethylphenyl)-, 4-methylbenzenesulfonate(1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(2,4-二甲基苯基)碘鎓对甲苯磺酸盐 | 2776240-91-4 | 9726733 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(5,6,7,8-tetrahydro-2-naphthalenyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(5,6,7,8-四氢萘-2-基)碘鎓对甲苯磺酸盐 | 2776242-00-1 | 9726734 |
| Iodonium, (3-bromo-4-methoxyphenyl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate(1:1) (ACI), 98% (3-溴-4-甲氧基苯基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776240-93-6 | 9726735 |
| Iodonium, (2-bromo-4,5-dimethylphenyl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (2-溴-4,5-二甲基苯基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-32-6 | 9726736 |
| Iodonium, [4-(4-bromophenoxy)phenyl](3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% [4-(4-溴苯氧基)苯基](3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-07-5 | 9726737 |
| Iodonium, (2-bromo-4,6-dimethoxyphenyl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (2-溴-4,6-二甲氧基苯基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776240-95-8 | 9726738 |
| Iodonium, [2-(cyanomethyl)-4-methoxyphenyl](3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% [2-(氰基甲基)-4-甲氧基苯基](3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776240-97-0 | 9726739 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)[4-methoxy-3-(methoxycarbonyl)phenyl]-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)[4-甲氧基-3-(甲氧基羰基)苯基]碘鎓对甲苯磺酸盐 | 2776240-99-2 | 9726740 |
| Iodonium, [3-(carboxymethyl)-4-methoxyphenyl](3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% 3−(羧甲基)−4−甲氧基苯基(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-01-9 | 9726741 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)[2,4,6-tris(1-methylethyl)phenyl]-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)[2,4,6-三(异丙基)苯基]碘鎓对甲苯磺酸盐 | 2776241-03-1 | 9726742 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(2-formyl-4,6-dimethoxyphenyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(2-甲酰基-4,6-二甲氧基苯基)碘鎓对甲苯磺酸盐 | 2776241-05-3 | 9726743 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)[4-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)[4-甲氧基-3-(4,4,5,5-四甲基-1,3,2-二氧杂硼杂环戊烷-2-基)苯基]碘鎓对甲苯磺酸盐 | 2776241-09-7 | 9726744 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)-2-thienyl-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(2-噻吩基)碘鎓对甲苯磺酸盐 | 2776241-10-0 | 9726745 |
| Iodonium, (5-acetyl-2-thienyl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (5-乙酰基-2-噻吩基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-12-2 | 9726746 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(1,3,5-trimethyl-1H-pyrazol-4-yl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(1,3,5-三甲基-1H-吡唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-14-4 | 9726747 |
| Iodonium, (2,6-dimethoxy-3-pyridinyl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (2,6-二甲氧基-3-吡啶基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-16-6 | 9726748 |
| Iodonium, (3,4-dibromo-2-thienyl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,4-二溴-2-噻吩基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-34-8 | 9726749 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(2-iodo-4-methoxyphenyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(2-碘-4-甲氧基苯基)碘鎓对甲苯磺酸盐 | 3087723-96-1 | 9726750 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)-9,9′-spirobi[9H-fluoren]-2-yl-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(9,9′-螺二[9H-芴]-2-基)碘鎓对甲苯磺酸盐 | 2971810-62-3 | 9726751 |
| Iodonium, (6,11-dihydro-11-oxodibenz[b,e]oxepin-2-yl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (6,11-二氢-11-氧代二苯并[b,e]氧杂环庚三烯-2-基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-22-4 | 9726752 |
| Iodonium, (9,10-dihydro-9,10[1′,2′]-benzenoanthracen-2-yl)(3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (9,10-二氢-9,10[1′,2′]-苯并蒽-2-基)(3,5-二甲基异噁唑-4-基)碘鎓对甲苯磺酸盐 | 2776241-18-8 | 9726753 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)(9-methoxy-7-oxo-7H-furo[3,2-g][1]benzopyran-4-yl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)(9-甲氧基-7-氧代-7H-呋喃并[3,2-g][1]苯并吡喃-4-基)碘鎓对甲苯磺酸盐 | 2776241-24-6 | 9726754 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)[2,6-dimethyl-4-[[(2-oxo-5-oxazolidinyl)methoxy]phenyl]-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)[2,6-二甲基-4-[[(2-氧代-5-噁唑烷基)甲氧基]苯基]碘鎓对甲苯磺酸盐 | 2776241-28-0 | 9726755 |
| Iodonium, [4-[[(4-carboxy-4-methylpentyl)oxy]-2,5-dimethylphenyl](3,5-dimethyl-4-isoxazolyl)-, 4-methylbenzenesulfonate (1:1) (ACI), 98% 4-[(4-羧基-4-甲基戊基)氧基]-2,5-二甲基苯基碘鎓对甲苯磺酸盐 | 2776241-26-8 | 9726756 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)[4-[[(5-ethoxy-4,4-dimethyl-5-oxopentyl)oxy]-2,5-dimethylphenyl]-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)[4-[[(5-乙氧基-4,4-二甲基-5-氧代戊基)氧基]-2,5-二甲基苯基]碘鎓对甲苯磺酸盐 | 3057843-14-5 | 9726757 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)[5-[[1,1-dimethyl-2-[[(3-phenoxyphenyl)methoxy]ethyl]-2-ethoxyphenyl]-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)[5-[[1,1-二甲基-2-[[(3-苯氧基苯基)甲氧基]乙基]-2-乙氧基苯基]碘鎓对甲苯磺酸盐 | 2776241-30-4 | 9726758 |
| Iodonium, (3,5-dimethyl-4-isoxazolyl)[5-(4-fluorophenyl)-2-thienyl]-, 4-methylbenzenesulfonate (1:1) (ACI), 98% (3,5-二甲基异噁唑-4-基)[5-(4-氟苯基)-2-噻吩基]碘鎓对甲苯磺酸盐 | 3087724-06-6 | 9726759 |
参考文献
- Qilong Lv , Yanchuan Zhao. Expanding the toolbox of C–H functionalization: the emergence of DMIX-substituted hypervalent iodine reagents. Tetrahedron Letters 177 (2026) 155979.
推荐阅读
C-H活化——麦克阿瑟天才奖获得者一年2篇ScienceC-H键活化试剂——有机合成的强有力工具
铑催化不对称 C-H 活化构建螺环丙烷骨架
