CAS 121584-52-9

Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V]

登记编号：Voclosporin-004

应用背景（按来源药适应症）

狼疮肾炎伏环孢素肾脏移植排斥伏环孢素新型冠状病毒感染伏环孢素系统性红斑狼疮伏环孢素局灶性节段性肾小球硬化症伏环孢素干眼综合征伏环孢素

来源药（使用该中间体的合成路线）

品种	梯队	到期年
伏环孢素Voclosporin	Tier C · 观察 / 贸易	-

合成路线中的位置（上下游链）

按路线登记顺序排列，左→右为合成方向；高亮为当前 CAS，其余可点击跳转对应档案。

伏环孢素优化路线步数：2总收率：/

Cyclo{-[4-( E)-but-2-enyl- N,4-dimethyl- L-threonyl]-L-homoalanyl-(N-methylglycyl)-( N-methyl-L-leucyl)-L-valyl-( N-me-thyl- L-leucyl)-L-alanyl- D-alanyl-(N-methyl-L-leucyl)-( N-methyl-L-leucyl)-(N-methyl-L-valyl)-}→(1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhex-4-en-1-ylacetate→(1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhex-4-en-1-ylbenzoate→Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V]→(1R,2R)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methyl-4-oxobutylbenzoate

伏环孢素优化路线步数：2总收率：9.6g(Voclosporin (Free))

Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V]→(1R,2R)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methyl-4-oxobutylbenzoate→Triphenyl(prop-2-en-1-yl)phosphoniumbromide→(1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhepta-4,6-dien-1-ylacetate→(1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhepta-4,6-dien-1-ylbenzoate→[Phenyl(prop-2-en-1-yl)phosphoroso]benzene→Dimethylallylphosphonate

伏环孢素优化路线步数：2总收率：14.09g(Voclosporin (Free))

Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V]→trimethyl[(1E)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)prop-1-en-1-yl]silane→(1R,2R,4R,5R)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-ethyl-14,32-diisopropyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-4-hydroxy-2-methyl-5-(trimethylsilyl)hept-6-en-1-ylacetate

伏环孢素优化路线步数：2总收率：4.92g(Voclosporin-004)

伏环孢素优化路线步数：2总收率：40mg(Voclosporin (Free))

Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V]→3-(Trimethylsilyl)propyne→(1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhepta-4,6-dien-1-ylacetate

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