1892-57-5

Basic information

• Product Name: 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide
• Synonyms: 1-ETHYL-3-(3-DIMETHYLAMINOPROPYL) CARBODIIMIDE;1-(3-DIMETHYLAMINOPROPYL)-3-ETHYLCARBODIIMIDE;EDAC;EDCI;WATER-SOLUBLE CARBODIIMIDE;WSCD;WSCI;N-ETHYL-N'-(3-DIMETHYLAMINOPROPYL)CARBODIIMIDE
• CAS NO: 1892-57-5
• Molecular Formula: C₈H₁₇N₃
• Molecular Weight: 155.24
• EINECS: 217-579-2
• Product Categories: straight chain compounds
• Mol File: 1892-57-5.mol

Chemical Properties

• Boiling Point: 66-68°C/1mm
• Flash Point: 66-68°C/1mm
• Appearance: Colorless to slightly yellow/Liquid
• Density: 0.877 g/mL at 20 °C(lit.)
• Refractive Index: n20/D 1.461
• Storage Temp.: −20°C
• Solubility: Chloroform
• PKA: 9.52±0.28(Predicted)
• Water Solubility: Soluble in water.
• Sensitive: Air Sensitive
• BRN: 507429
• CAS DataBase Reference: 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide(1892-57-5)
• EPA Substance Registry System: 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide(1892-57-5)

Safety Data

• Hazard Codes: C
• Statements: 34
• Safety Statements: 26-36/37/39-45
• RIDADR: UN 2735 8/PG 3
• WGK Germany: 3
• F: 1-3-10
• TSCA: Yes
• HazardClass: 8
• PackingGroup: III
• Hazardous Substances Data: 1892-57-5(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
1-(3-Dimethylaminopropyl)-3-Ethylcarbodiimide is used as a carboxyl activating agent for the synthesis of peptides, which are crucial components in the development of various drugs and therapies. It is also employed in the activation of phosphate groups in phospho mono and di esters, which are vital in the creation of 3'-amino-3'-deoxyadenosine-5'-diand triphosphates, essential molecules in molecular biology and genetics.
Used in Biotechnology Industry:
In the biotechnology sector, 1-(3-Dimethylaminopropyl)-3-Ethylcarbodiimide plays a vital role in the immobilization of large biomolecules, such as enzymes and proteins, in association with N-hydroxysuccinimide. This process is essential for the development of biosensors, biocatalysts, and other biotechnological applications.
Used in Immunology and Diagnostics:
1-(3-Dimethylaminopropyl)-3-Ethylcarbodiimide is used in the preparation of antibodies, specifically immunoconjugates, which are essential tools in immunology and diagnostics. These immunoconjugates are used for the detection, quantification, and manipulation of specific target molecules, such as antigens or other biological markers.
Used in Chemical Synthesis:
In the field of chemical synthesis, 1-(3-Dimethylaminopropyl)-3-Ethylcarbodiimide is employed in the acylation of phosphoranes, which are important intermediates in the synthesis of various organic compounds and pharmaceuticals.
Overall, 1-(3-Dimethylaminopropyl)-3-Ethylcarbodiimide is a versatile compound with applications across multiple industries, including pharmaceuticals, biotechnology, immunology, diagnostics, and chemical synthesis, due to its ability to activate carboxyl and phosphate groups, as well as its role in the immobilization of biomolecules and the synthesis of various compounds.

Synthetic route

1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (32897-26-0) → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
With triethylamine; p-toluenesulfonyl chloride In dichloromethane for 4h; Heating;	60%

1-(3-dimethylamino-propyl)-3-ethyl-thiourea → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
With dicarbonyl(cyclopentadienyl)methyliron(II); Triethoxysilane In tetrahydrofuran; 1,3,5-trimethyl-benzene at 60℃; for 24h; Schlenk technique; Inert atmosphere;	46%
With sodium hypochlorite; ethylenediaminetetraacetic acid at 30℃; Reagent/catalyst; Temperature;
With bis(trichloromethyl) carbonate In Petroleum ether at 15 - 45℃; for 3h; Temperature;	213.6 g

Ethyl isothiocyanate (542-85-8) + 1-amino-3-(dimethylamino)propane (109-55-7) → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
(i) Et2O, (ii) HgO, benzene; Multistep reaction;
(i) Et2O, (ii) HgO, CH2Cl2; Multistep reaction;

1-amino-3-(dimethylamino)propane (109-55-7) + ethyl isocyanate (109-90-0) → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
(i), (ii) TsCl; Multistep reaction;

1-amino-3-(dimethylamino)propane (109-55-7) + (+-)-ethoxycarbonylamino-phenyl-acetic acid ethyl ester → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
Multi-step reaction with 2 steps 1: diethyl ether / 2 h / Ambient temperature 2: 60 percent / triethylamine, toluenesulfonyl chloride / CH2Cl2 / 4 h / Heating View Scheme

1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride (25952-53-8) → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
With potassium carbonate In trifluoromethylbenzene (BTF); water

N-(3-Dimethylamino-propyl)-dithiocarbamidsaeure (18997-72-3) → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
Multi-step reaction with 3 steps 1: chloroformic acid ethyl ester; triethylamine / dichloromethane / 3 h / 10 - 15 °C 2: dichloromethane / 1 h / 10 - 15 °C 3: sodium hypochlorite; ethylenediaminetetraacetic acid / 30 °C View Scheme

3-(dimethylamino)propyl isothiocyanate (27421-70-1) → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
Multi-step reaction with 2 steps 1: dichloromethane / 1 h / 10 - 15 °C 2: sodium hypochlorite; ethylenediaminetetraacetic acid / 30 °C View Scheme

1-amino-3-(dimethylamino)propane (109-55-7) → N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5)

Conditions	Yield
Multi-step reaction with 4 steps 1: methanol / 2 h / 10 - 20 °C 2: chloroformic acid ethyl ester; triethylamine / dichloromethane / 3 h / 10 - 15 °C 3: dichloromethane / 1 h / 10 - 15 °C 4: sodium hypochlorite; ethylenediaminetetraacetic acid / 30 °C View Scheme

ferrocenecarboxylic acid (1271-42-7) + methyl (2S)-2-amino-3-hydroxypropanoate hydrochloride (5680-80-8) + benzotriazol-1-ol (2592-95-2) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → Fe(C5H5)(C5H4)CONHCH(CH2OH)COOCH3

Conditions	Yield
With CuCl In N,N-dimethyl-formamide	99%

morphine-6-hemisuccinate (36507-55-8) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → EDC-morphine-6-hemisuccinate

Conditions	Yield
With hydrogenchloride In water at 37℃; for 2h; pH=5.5;	98%

L-aspartic acid di-tert-butyl ester hydrochloride + Z-MeVal-OH (42417-65-2) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) + 1-hydroxybenzotriazol-hydrate (80029-43-2, 123333-53-9) → N-[N-(benzyloxycarbonyl)-N-methylvalyl]-L-aspartic acid di-tert-butyl ester

Conditions	Yield
With triethylamine In tetrahydrofuran	98%

hyaluronic acid sodium salt from bacterial source (100 kDa) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → hyaluronyl N-[3-(dimethylamino)propyl]-N’-ethylimidocarbamate, content of isoureido residues 100%

Conditions	Yield
With hydrogenchloride In water at 20℃; for 2h; pH=4.7 - 4.8;	98%

bis(bis(trimethylsilyl)amido)tin(II) (55147-78-9) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → [(C2H5NC(N(Si(CH3)3)2)N(CH2)3N(CH3)2)2Sn] (1362855-87-5)

Conditions	Yield
In diethyl ether (Ar); C2H5NCN(CH2)3N(CH3)2 in Et2O added to a soln. of Sn compd. at roomtemp., stirred for 0.5 h; filtered, evapd. (vac.); obtained oily; elem. anal.;	96%

butane-1-sulfonic acid (2386-47-2) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide n-butylsulfonate

Conditions	Yield
at 15 - 25℃; for 1h; Large scale;	95.8%

methanesulfonic acid (75-75-2) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide methanesulfonate

Conditions	Yield
at 15 - 25℃; for 1h; Large scale;	95.5%

1-hydroxy-pyrrolidine-2,5-dione (6066-82-6) + 25-hydroxyvitamin D3-3-hemisuccinate + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → methacrylic acid N-hydroxysuccinimide ester (38862-25-8)

Conditions	Yield
With sodium sulfate In dichloromethane	94%

dibenzyl L-aspartate toluene-4-sulphonate (2886-33-1) + 1-<(tert-butyloxy)carbonylamino>cyclopropane-1-carboxylic acid (88950-64-5) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → 1-[(tert-butoxycarbonyl)amino]cyclopropanecarbonyl-L-aspartic acid dibenzyl ester (1415763-45-9)

Conditions	Yield
With hydrogenchloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine In dichloromethane	94%

hexadecane-1-sulfonic acid (6140-88-1) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide cetyl sulfonate

Conditions	Yield
at 15 - 25℃; for 1h; Large scale;	94%

2-(tert-butoxycarbonylamino)-3-phenylpropionic acid (4530-18-1) + [Ru(η(5)-C5Me5)(phenylalanine methyl ester)]Cl + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → [Ru(η(5)-C5Me5)(PhCH2CH(NHCOOBu(t))CONHCH(CO2H)CH2Ph)]Cl

Conditions	Yield
With triethylamine In dichloromethane addn. of 1 equiv. protected phenylalanine ester to Ru-complex, then addn. of Et3N and carbodiimide derivative, stirring at -50°C for 12 h; addn. of water, citric acid and Na2CO3, solvent removal; elem. anal.;	92%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) + fluoren-9-ylidene-hydrazine (13629-22-6) → EtNHC(NNfluoren)NHCH2CH2CH2NMe2 (1445265-19-9)

Conditions	Yield
With [Ti(pentamethylcyclopentadienyl)(N(xylyl)C4H6N)(tert-butylimido)(tert-butylamine)] In 1,4-dioxane at 80℃; for 24h; Reagent/catalyst; Inert atmosphere; Schlenk technique;	92%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride (25952-53-8)

Conditions	Yield
With triethylamine hydrochloride In acetonitrile at 15℃; for 1h; Temperature;	92%

(Sp)-ortho-(diphenylphosphanyl)ferrocenylcarboxylic acid (677722-99-5, 847675-62-1, 297176-74-0) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → N-[3-(dimethylamino)propyl]-N'-ethyl-N-[(Sp)-2-(diphenylphosphino)ferrocenecarbonyl]urea

Conditions	Yield
In dichloromethane (Ar); carbodiimide was added to soln. of Fe complex in CH2Cl2; stirred at room temp. for 20 h; evapd. (vac.); chromd. (silica gel, CH2Cl2/MeOH, 10/1 to 5/1); evapd. (vac.);	91%

bis(bis(trimethylsilyl)amido)tin(II) (55147-78-9) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → (C2H5NC(N(Si(CH3)3)2)N(CH2)3N(CH3)2)SnN(SiMe3)2 (1362855-81-9)

Conditions	Yield
In diethyl ether (Ar); a soln. of C2H5NCN(CH2)3N(CH3)2 added to a soln. of Sn compd. at room temp., stirred for 2 h; filtered, evapd. (vac.); obtained oily; elem. anal.;	91%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) + 2,4-dinitrobenzoic acid (610-30-0) → (3-(3-(dimethylamino)propyl)-1-ethyl-6-nitro-2,4-dioxo-1,3-diazaspiro[4.5]deca-6,9-dien-1-ium-8-ylidene)azinate

Conditions	Yield
Stage #1: N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; 2,4-dinitrobenzoic acid In dichloromethane at 20℃; for 0.5h; Stage #2: With N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 16h;	91%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) + biotinyl-bromoacetyl hydrazide → 1-ethyl-3-{3-[(biotinylhydrazinocarbonylmethyl)dimethylammonio]propyl}carbodiimide bromide

Conditions	Yield
In N,N-dimethyl-formamide for 1h; Ambient temperature;	90%

[bis(trimethylsilyl)amino]tin chloride dimer + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → [(C2H5NC(N(Si(CH3)3)2)N(CH2)3N(CH3)2)SnCl] (1362855-85-3)

Conditions	Yield
In diethyl ether (Ar); C2H5NCN(CH2)3N(CH3)2 in Et2O added to a suspn. of Sn compd. at room temp., stirred; filtered, evapd. (vac.); obtained oily; elem. anal.;	90%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) + N,N,N',N'-tetramethylguanidine (80-70-6) → C13H30N6 (1542158-74-6)

Conditions	Yield
at 120℃; for 0.0833333h; Inert atmosphere; Microwave irradiation; Green chemistry;	89%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) + 1,1-bis(4-bromophenyl)hydrazine (5149-08-6) → EtNHC{NN(p-BrC6H4)2}NHCH2CH2CH2NMe2

Conditions	Yield
With [Ti(pentamethylcyclopentadienyl)(N(xylyl)C4H6N)(tert-butylimido)(tert-butylamine)] In toluene at 105℃; for 24h; Reagent/catalyst; Inert atmosphere; Schlenk technique;	87%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) + methyl iodide (74-88-4) → 1-[3-(dimethylamino)-propyl]-3-ethylcarbodiimide methiodide (138551-31-2)

Conditions	Yield
In diethyl ether for 48h; Ambient temperature;	85%
In dichloromethane at 15 - 25℃; for 1h; Large scale;	81.2%

L-glutamic acid di-tert-butyl ester hydrochloride + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → N-({2-[(4-amidino-2-fluorophenoxy)carbonyl]-4,5-dihydrothieno[2,3-c]pyridin-6(7H)-yl}acetyl)-L-glutamic acid bis(trifluoroacetate)

Conditions	Yield
In pyridine; trifluoroacetic acid	83%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) + methyl iodide (74-88-4) → 3-{[(ethylimino)methylene]-amino}-N,N,N-trimethyl-1-propanaminium iodide (22572-40-3)

Conditions	Yield
In dichloromethane at 15 - 25℃; for 1h; Industrial scale;	81.2%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → N-allyl-N-(3-{5-[(4-amidinophenoxy)carbonyl]-3-methylthiophen-2-yl}propanoyl)glycine trifluoroacetate (1415763-66-4)

Conditions	Yield
With trifluoroacetic acid In pyridine	81%

N-BOC-1,2-diaminoethane (57260-73-8) + 4-carboxy-3-hydroxyphenyl azide (66761-27-1) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → [2-(4-azido-2-hydroxy-benzoylamino)-ethyl]-carbamicacid tert-butyl ester (1293988-98-3)

Conditions	Yield
Stage #1: 4-carboxy-3-hydroxyphenyl azide; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide With benzotriazol-1-ol In N,N-dimethyl-formamide at 20℃; for 0.5h; Inert atmosphere; Stage #2: N-BOC-1,2-diaminoethane In N,N-dimethyl-formamide at 20℃; for 18h; Inert atmosphere;	75%

2-amino-5-bromonicotinicacid (52833-94-0) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → 2-amino-5-bromo-N-isopropylpyridine-3-carboxamide

Conditions	Yield
Stage #1: 2-amino-5-bromonicotinicacid; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide With benzotriazol-1-ol In tetrahydrofuran at 0℃; for 0.25h; Stage #2: With isopropylamine In tetrahydrofuran at 20℃;	75%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → N-allyl-N-({2-[(2,2,2-trichloroethoxy)carbonyl]-4,5-dihydrothieno[2,3-c]pyridin-6(7H)-yl}acetyl)-L-glutamic acid di-tert-butyl ester (1415763-54-0)

Conditions	Yield
With trifluoroacetic acid In pyridine	74%

L-aspartic acid di-tert-butyl ester hydrochloride + N-{[5-(4-amidinophenoxycarbonyl)furan-2-yl]methyl}-D-proline bis(trifluoroacetate) + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → N-(N-{[5-(4-amidinophenoxycarbonyl)furan-2-yl]methyl}-D-prolyl)-L-aspartic acid di-tert-butyl ester bis(trifluoroacetate)

Conditions	Yield
With pyridine; trifluoroacetic acid	73%

N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → N-allyl-N-[N-allyl-N-(3-{5-[(4-amidinophenoxy)carbonyl]-3-methylthiophen-2-yl}propanoyl)glycyl]-L-glutamic acid trifluoroacetate (1415763-00-6)

Conditions	Yield
With trifluoroacetic acid In pyridine	73%

maleimide-PEG8-acid + C69H88N10O19 + N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (1892-57-5) → C95H130N12O31

Conditions	Yield
In chloroform for 1.5h;	72%

Upstream product

• 542-85-8 Ethyl isothiocyanate 
• 109-55-7 1-amino-3-(dimethylamino)propane 
• 109-90-0 ethyl isocyanate 
• 32897-26-0 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide 
• 25952-53-8 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride 
• 27421-70-1 3-(dimethylamino)propyl isothiocyanate 
• 18997-72-3 N-(3-Dimethylamino-propyl)-dithiocarbamidsaeure 

Downstream Products

• 175527-01-2 benzyl 2(R)-[(4-methoxybenzenesulfonyl)(benzyl)amino]-2[(N-dimethylaminoacetyl)-4-piperidinyl]acetate 
• 169547-22-2 [N-(3,5-dimethylbenzoyl)-N-methyl-3-[4-(5-isoxazolyl)-phenyl]-(D)-alanyl]-(L)-tryptophane methyl ester 
• 198894-70-1 N-[trans-4-(4-phenylpiperidin-1-ylmethyl)-1-cyclohexylmethyl]-5-thia-1,8b-diazaacenaphthylene-4-carboxamide 
• 81409-90-7 cabergoline 
• 89973-67-1 trans-PdCl₂(Gly-L-PheOEt)2 
• 105944-46-5 cis-PdCl₂(L-His-L-PheOEt) 
• 105944-43-2 trans-PdCl₂(L-Leu-L-PheOEt)2*H₂O 
• 1032527-82-4 tert-butyl (1-{4-[3-(ethylamino)-9-phenyl[1,2,4]triazolo[3,4-f]-1,6-naphthyridin-8-yl]phenyl}cyclobutyl)carbamate 
• 1445264-94-7 EtNHC(NNMePh)NHCH₂CH₂CH₂NMe₂ 

Relevant articles and documents

Insights into Fast Amide Couplings in Aqueous Nanomicelles

1-Ethyl-3-(3-(dimethylamino)propyl)-carbodiimide (EDC?HCl) has both lipophilic and hydrophilic regions, causing self-aggregation (also called nanoparticle formation) in an aqueous medium containing PS-750-M amphiphile. Kinetic and proton nuclear magnetic resonance studies were used to probe the effect of different organic bases on the potential nanoparticle formation of EDC?HCl. It also reveals why the pyridine base works better under micellar conditions. The methodology was examined on the multigram scale synthesis of bioactive molecules, where excellent reaction yields were obtained without product epimerization while maintaining a shorter reaction time.

1 - Ethyl - (3 - dimethyl aminopropyl) carbodiimide hydrochloride preparation method (by machine translation)

The invention relates to a 1 - ethyl - (3 - dimethyl aminopropyl) carbodiimide hydrochloride preparation method, which belongs to the technical field of pharmaceutical intermediates. The preparation method comprises the reaction generating EDTC, prepared crude EITC, distillation fractionation, to produce an intermediate, make the EDC and to obtain the target product in seven steps. The present invention provides a preparation method, has a high product yield and purity, the operation step is simple, easy to implement, for industrial production. (by machine translation)

A method of manufacturing a carbodiimide compound

PROBLEM TO BE SOLVED: To provide a novel method that can efficiently produce a carbodiimide compound without using substances that are harmful, hazardous, expensive, or difficult to obtain.SOLUTION: The method of producing a carbodiimide compound includes converting a thiourea compound having a specific structure to a carbodiimide compound having a specific structure in the presence of at least one of an iron compound and a molybdenum compound.

1 - (3-dimethylamino-propyl) - 3-ethyl carbodiimide hydrochloride preparation method

The invention belongs to the field of organic chemical industry, and particularly relates to a preparation method of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride. The method comprises the following steps: enabling N,N'-dimethyl-1,3-propanediamine and carbon disulfide as raw materials to react in an organic solvent to generate an intermediate 1; enabling the intermediate 1 and ethyl chloroformate to react in the organic solvent, and preparing an intermediate 2 from triethylamine as an acid-binding agent; enabling the intermediate 2 and ethylamine to react in the organic solvent, so as to prepare an intermediate 3; adding a catalyst to the intermediate 3, oxidizing one time with an oxidant, so as to obtain a crude product 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, extracting and separating, so as to obtain an intermediate 4; and carrying out salt exchange reaction on the intermediate 4 and hydrochloride, so as to prepare the product 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride. The method has the advantages of relatively high conversion rate and relatively high total recovery rate and is simple to operate and suitable for industrial production.

Dehydrogenative desulfurization of thiourea derivatives to give carbodiimides, using hydrosilane and an iron complex

Dehydrogenative desulfurization of thiourea derivatives (RNHC(S)NHR′) has been achieved, to give carbodiimides (RNCNR′), in the reaction with hydrosilane and (η5-C5H5)Fe(CO) 2Me. The obtained carbodiimide reacted with (η5-C 5H5)Fe(CO)(SiR3) formed in the reaction to give an N-silylated η2-amidino iron complex, which was isolated and then characterized by X-ray analysis.

Production of Cabergoline and Novel Polymorphic Form Thereof

The present application relates to a novel polymorphic form of cabergoline comprising cabergoline and t-amyl methyl ether, designated Form TAME cabergoline, together with a novel method of producing cabergoline.