CAS 107-15-3

ethane-1,2-diamineEthane-1,2-diamine1,2-Diaminoethane

Codes: PEGL-006, Oxymetazoline Hydrochloride-010, (IV)122568-1-a, (II)122568-2-a, (VIII)122568-3-a

Application context (from source-drug indications)

Type 2 diabetesPEG-LoxenatideObesityPEG-LoxenatideEndometrial hyperplasiaPEG-LoxenatideAnaesthesiaOxymetazoline Hydrochloride/Tetracaine HydrochloridePeriapical periodontitisOxymetazoline Hydrochloride/Tetracaine HydrochlorideDental cariesOxymetazoline Hydrochloride/Tetracaine HydrochlorideAttention deficit hyperactivity disorderClonidine Hydrochloride (Tris Pharma)HypertensionClonidine Hydrochloride (Tris Pharma)Nasal congestionOxymetazoline HydrochlorideCongestionOxymetazoline HydrochloridePtosisOxymetazoline HydrochlorideFunctional faecal incontinenceOxymetazoline HydrochlorideRosaceaOxymetazoline HydrochlorideRashOxymetazoline Hydrochloride

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
PEG-Loxenatide	Tier C — Watch / trade	-
Oxymetazoline Hydrochloride/Tetracaine Hydrochloride	Tier C — Watch / trade	-
Clonidine Hydrochloride (Tris Pharma)	Tier C — Watch / trade	-
Oxymetazoline Hydrochloride	Tier C — Watch / trade	-

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.

PEG-LoxenatideOriginator routesteps: 7total yield: 4.50 g (PEG-Loxenatide)

2-(2-methoxyethoxy)ethan-1-ol→2-(2-methoxyethoxy)ethyl carbonochloridate→2,5-dioxopyrrolidin-1-yl (2-(2-methoxyethoxy)ethyl) carbonate→15-(((2-(2-methoxyethoxy)ethoxy)carbonyl)amino)-9-oxo-2,5,8-trioxa-10-azahexadecan-16-oic acid→2,5-dioxopyrrolidin-1-yl 15-(((2-(2-methoxyethoxy)ethoxy)carbonyl)amino)-9-oxo-2,5,8-trioxa-10-azahexadecan-16-oate→ethane-1,2-diamine→bis(2-(2-methoxyethoxy)ethyl) (6-((2-aminoethyl)amino)-6-oxohexane-1,5-diyl)dicarbamate→4-nitrophenyl 3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanoate→bis(2-(2-methoxyethoxy)ethyl) (6-((2-(3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanamido)ethyl)amino)-6-oxohexane-1,5-diyl)dicarbamate

Oxymetazoline Hydrochloride/Tetracaine HydrochlorideOptimised routesteps: 6total yield: 26g(Oxymetazoline hydrochloride (API))

(4-tert-Butyl-3-hydroxy-2,6-dimethylphenyl)acetonitrile→Ethane-1,2-diamine→N-[2-(Acetamido)ethyl]acetamide→6-tert-Butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol→(4-tert-Butyl-3-hydroxy-2,6-dimethylphenyl)acetyl chloride→(4-tert-Butyl-3-hydroxy-2,6-dimethylphenyl)acetic acid→Ethane-1,2-diamine 4-methylbenzenesulfonate→2-(4-tert-Butyl-3-hydroxy-2,6-dimethylphenyl)acetamide→2-Bromoethanamine hydrobromide→Ethylene dibromide→Ethyl 2-(4-tert-butyl-3-hydroxy-2,6-dimethylphenyl)ethanimidoate hydrochloride

Clonidine Hydrochloride (Tris Pharma)Optimised routesteps: 3total yield: /

2,6-Dichloroaniline→(2,6-dichlorophenyl)thiourea→N-[(2,6-Dichlorophenyl)carbamothioyl]benzamide→Methyl N-(2,6-dichlorophenyl)carbamimidothioate hydrogen iodide→1,2-Diaminoethane

Clonidine Hydrochloride (Tris Pharma)Optimised routesteps: 2total yield: /

1,3-Dichloro-2-isothiocyanatobenzene→1,2-Diaminoethane→3-(2-aminoethyl)-1-(2,6-dichlorophenyl)thiourea

Clonidine Hydrochloride (Tris Pharma)Optimised routesteps: 4total yield: /

1-Chloro-2-nitrobenzene→N-(2-chlorophenyl)hydroxylamine→Formic acid→N-(2-Chlorophenyl)-N-hydroxyformamide→2,6-Dichloroaniline→N-(2,6-Dichlorophenyl)formamide→1,2-Diaminoethane

Oxymetazoline HydrochlorideOptimised routesteps: 6total yield: 26g(Oxymetazoline hydrochloride (API))

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