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CAS 4254-14-2

(R)-1,2-PropanediolPropane-1,2(R)-diol

Codes：Tenofovir disoproxil phosphate-017

Application context (from source-drug indications)

HIV感染拉米夫定/富马酸替诺福韦二吡呋酯慢性乙型肝炎拉米夫定/富马酸替诺福韦二吡呋酯HIV感染依非韦伦/拉米夫定/富马酸替诺福韦二吡呋酯HIV感染恩曲他滨/盐酸利匹韦林/富马酸替诺福韦二吡呋酯

Source drugs (routes using this intermediate)

DrugTierExpiry
拉米夫定/富马酸替诺福韦二吡呋酯Lamivudine/Tenofovir Disoproxil FumarateTier C — Watch / trade-
依非韦伦/拉米夫定/富马酸替诺福韦二吡呋酯Efavirenz/Lamivudine/Tenofovir Disoproxil FumarateTier C — Watch / trade-
恩曲他滨/盐酸利匹韦林/富马酸替诺福韦二吡呋酯Emtricitabine/Rilpivirine Hydrochloride/Tenofovir Disoproxil FumarateTier B — Position early-

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

拉米夫定/富马酸替诺福韦二吡呋酯优化路线steps: 11total yield: 23.3g(Tenofovir disoproxil phosphate (API))
Chloroacetyl chloride→1-Chloro-2(R)-propanol→Diethyl (tosyloxy)methylphosphonate→Diethyl (chloromethyl)phosphonate→Diethyl phosphonate→Diethyl phosphonomethanol→Diethyl (2-chloro-1(R)-methylethoxy)methylphosphonate→6-Aminopurine→(R)-9-[2-(Diethylphosphonomethoxy)propyl] adenine→(R)-9-(2-Phosphonomethoxypropyl)adenine→Chloromethyl isopropyl carbonate→Bis[[(isopropoxycarbonyl)oxy]methyl] ([[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy]methyl)phosphonate→2(R)-Methyloxirane→(R)-(+)-9-(2-Hydroxypropyl)adenine→(R)-Propylene carbonate→(S)-Glycidol→(R)-1,2-Propanediol
拉米夫定/富马酸替诺福韦二吡呋酯优化路线steps: 8total yield: 1.97g(Tenofovir disoproxil phosphate-013)
2(R)-Methyloxirane→(R)-1,2-Propanediol→2(S)-Hydroxypropionic acid→Methyl (2S)-2-hydroxypropanoate→Methyl (2S)-2-[(methanesulfonyl)oxy]propanoate→(2S)-1-Hydroxypropan-2-yl methanesulfonate→(2R)-2-Hydroxypropanoic acid→D-Lactic acid methyl ester→(2R)-2-Hydroxypropyl 4-methylbenzene-1-sulfonate
拉米夫定/富马酸替诺福韦二吡呋酯优化路线steps: 4total yield: /
Propane-1,2(R)-diol→(4R)-4-Methyl-1,3-dioxolane→N,N,N',N'-Tetraethylphosphorodiamidous chloride→P-([[(2R)-1-Chloropropan-2-yl]oxy]methyl)-N,N,N',N'-tetraethylphosphonic diamide→6-Aminopurine→P-([[(2R)-1-(6-Amino-9H-purin-9-yl)propan-2-yl]oxy]methyl)-N,N,N',N'-tetraethylphosphonic diamide
依非韦伦/拉米夫定/富马酸替诺福韦二吡呋酯优化路线steps: 11total yield: 23.3g(Tenofovir disoproxil phosphate (API))
Chloroacetyl chloride→1-Chloro-2(R)-propanol→Diethyl (tosyloxy)methylphosphonate→Diethyl (chloromethyl)phosphonate→Diethyl phosphonate→Diethyl phosphonomethanol→Diethyl (2-chloro-1(R)-methylethoxy)methylphosphonate→6-Aminopurine→(R)-9-[2-(Diethylphosphonomethoxy)propyl] adenine→(R)-9-(2-Phosphonomethoxypropyl)adenine→Chloromethyl isopropyl carbonate→Bis[[(isopropoxycarbonyl)oxy]methyl] ([[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy]methyl)phosphonate→2(R)-Methyloxirane→(R)-(+)-9-(2-Hydroxypropyl)adenine→(R)-Propylene carbonate→(S)-Glycidol→(R)-1,2-Propanediol
依非韦伦/拉米夫定/富马酸替诺福韦二吡呋酯优化路线steps: 8total yield: 1.97g(Tenofovir disoproxil phosphate-013)
2(R)-Methyloxirane→(R)-1,2-Propanediol→2(S)-Hydroxypropionic acid→Methyl (2S)-2-hydroxypropanoate→Methyl (2S)-2-[(methanesulfonyl)oxy]propanoate→(2S)-1-Hydroxypropan-2-yl methanesulfonate→(2R)-2-Hydroxypropanoic acid→D-Lactic acid methyl ester→(2R)-2-Hydroxypropyl 4-methylbenzene-1-sulfonate
依非韦伦/拉米夫定/富马酸替诺福韦二吡呋酯优化路线steps: 4total yield: /
Propane-1,2(R)-diol→(4R)-4-Methyl-1,3-dioxolane→N,N,N',N'-Tetraethylphosphorodiamidous chloride→P-([[(2R)-1-Chloropropan-2-yl]oxy]methyl)-N,N,N',N'-tetraethylphosphonic diamide→6-Aminopurine→P-([[(2R)-1-(6-Amino-9H-purin-9-yl)propan-2-yl]oxy]methyl)-N,N,N',N'-tetraethylphosphonic diamide
恩曲他滨/盐酸利匹韦林/富马酸替诺福韦二吡呋酯优化路线steps: 11total yield: 23.3g(Tenofovir disoproxil phosphate (API))
Chloroacetyl chloride→1-Chloro-2(R)-propanol→Diethyl (tosyloxy)methylphosphonate→Diethyl (chloromethyl)phosphonate→Diethyl phosphonate→Diethyl phosphonomethanol→Diethyl (2-chloro-1(R)-methylethoxy)methylphosphonate→6-Aminopurine→(R)-9-[2-(Diethylphosphonomethoxy)propyl] adenine→(R)-9-(2-Phosphonomethoxypropyl)adenine→Chloromethyl isopropyl carbonate→Bis[[(isopropoxycarbonyl)oxy]methyl] ([[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy]methyl)phosphonate→2(R)-Methyloxirane→(R)-(+)-9-(2-Hydroxypropyl)adenine→(R)-Propylene carbonate→(S)-Glycidol→(R)-1,2-Propanediol
恩曲他滨/盐酸利匹韦林/富马酸替诺福韦二吡呋酯优化路线steps: 8total yield: 1.97g(Tenofovir disoproxil phosphate-013)
2(R)-Methyloxirane→(R)-1,2-Propanediol→2(S)-Hydroxypropionic acid→Methyl (2S)-2-hydroxypropanoate→Methyl (2S)-2-[(methanesulfonyl)oxy]propanoate→(2S)-1-Hydroxypropan-2-yl methanesulfonate→(2R)-2-Hydroxypropanoic acid→D-Lactic acid methyl ester→(2R)-2-Hydroxypropyl 4-methylbenzene-1-sulfonate
恩曲他滨/盐酸利匹韦林/富马酸替诺福韦二吡呋酯优化路线steps: 4total yield: /
Propane-1,2(R)-diol→(4R)-4-Methyl-1,3-dioxolane→N,N,N',N'-Tetraethylphosphorodiamidous chloride→P-([[(2R)-1-Chloropropan-2-yl]oxy]methyl)-N,N,N',N'-tetraethylphosphonic diamide→6-Aminopurine→P-([[(2R)-1-(6-Amino-9H-purin-9-yl)propan-2-yl]oxy]methyl)-N,N,N',N'-tetraethylphosphonic diamide

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