59703-00-3

Basic information

• Product Name: 4-Ethyl-2,3-dioxo-1-piperazine carbonyl chloride
• Synonyms: edpc;1-CHLOROCARBONYL-4-ETHYL-2,3-DIOXOPIPERAZINE;4-ETHYL-2,3-DIOXO-1-PIPERAZINECARBONYL CHLORIDE;4-ETHYL-2,3-DIOXO-PIPERAZINE-1-CARBONYL CHLORIDE;4-ETHYL-2,3-DIOXO-PIPERAZINE CARBONYL CHLORIDE;N-Ethyl-2,3-dioxypiperazine-1-carbonylchloride;N-Ethyl-2,3-dioxo-1-piperazinecarbonyl chloride;4-Ethyl-2,3-dioxo-1-piperazine carbonyl chlorides
• CAS NO: 59703-00-3
• Molecular Formula: C7H9ClN2O3
• Molecular Weight: 204.61
• EINECS: 261-867-0
• Product Categories: Piperaizine;Piperazine derivates;Cefoperazone;API Intermediate
• Mol File: 59703-00-3.mol
• Article Data: 6

Chemical Properties

• Melting Point: 100 °C
• Boiling Point: 292.9 °C at 760 mmHg
• Flash Point: 131 °C
• Appearance: White to tan powder, partially agglomerated
• Density: 1.408 g/cm³
• Vapor Pressure: 0.00178mmHg at 25°C
• Refractive Index: 1.525
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• PKA: -1.81±0.20(Predicted)
• Water Solubility: decomposes
• CAS DataBase Reference: 4-Ethyl-2,3-dioxo-1-piperazine carbonyl chloride(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Ethyl-2,3-dioxo-1-piperazine carbonyl chloride(59703-00-3)
• EPA Substance Registry System: 4-Ethyl-2,3-dioxo-1-piperazine carbonyl chloride(59703-00-3)

Safety Data

• Hazard Codes: C
• Statements: 34
• Safety Statements: 45-36/37/39-26
• Hazardous Substances Data: 59703-00-3(Hazardous Substances Data)

Usage

Chemical Properties

White to tan powder, partially agglomerated

InChI:InChI=1/C7H9ClN2O3/c1-2-9-3-4-10(7(8)13)6(12)5(9)11/h2-4H2,1H3

Synthetic route

bis(trichloromethyl) carbonate (32315-10-9) + 1-ethyl-2,3-dioxo-piperazine (59702-31-7) → 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3)

Conditions	Yield
With pyridine; dmap; chloro-trimethyl-silane In dichloromethane at -25 - -20℃;	94.3%
With 1,8-diazabicyclo[5.4.0]undec-7-ene In dichloromethane at 10 - 20℃; for 1.06667h; Temperature; Reagent/catalyst; Green chemistry;	93.9%
Stage #1: 1-ethyl-2,3-dioxo-piperazine With chloro-trimethyl-silane; triethylamine In dichloromethane at 0 - 20℃; for 1h; Inert atmosphere; Schlenk technique; Stage #2: bis(trichloromethyl) carbonate In dichloromethane at -30℃; Inert atmosphere; Schlenk technique;

phosgene (75-44-5) + 1-ethyl-2,3-dioxo-piperazine (59702-31-7) → 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3)

Conditions	Yield
With chloro-trimethyl-silane; triethylamine In tetrahydrofuran; 1,4-dioxane

2-Mercaptobenzothiazole (149-30-4) → S-2-benzothiazolyl-4-ethyl-2,3-dioxo-1-piperazinethio-carboxylate (120600-74-0) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3)

Conditions	Yield
With triethylamine In dichloromethane

ampicillin (69-53-4) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → piperacillin (61477-96-1, 64131-97-1)

Conditions	Yield
With calcium carbonate In dichloromethane; water; ethyl acetate at 30 - 35℃; for 0.833333h;	93.7%
With sodium acetate; 1,8-diazabicyclo[5.4.0]undec-7-ene In dichloromethane; water; ethyl acetate at 5 - 10℃; for 0.916667h; pH=6.5 - 7.5; Temperature; Reagent/catalyst; Green chemistry;	92.8%
With triethylamine In water; ethyl acetate at 15 - 20℃; for 1h; pH=7.1;	123.5 g

7β-<(2R)-2-phenyl-2-amino>acetylamino-1-carba-1-dethia-3-cephem-4-carboxylic acid (72292-40-1, 72345-50-7, 72377-68-5) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → 7β-<(2R)-2-phenyl-2-(4-ethyl-2,3-dioxopiperazine-1-yl-carbonyl)amino>acetylamino-1-carba-1-dethia-3-cephem-4-carboxylic acid (72292-42-3, 72401-86-6)

Conditions	Yield
	93%

3-Methyl-4-isopropylphenol (3228-02-2) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → 4-isopropyl-3-methylphenyl N-(4-ethyl-2,3-dioxo-1-piperazine)carbamate

Conditions	Yield
With triethylamine In acetonitrile at 20℃; for 4h;	92%

D-Threonine (632-20-2) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → C11H17N3O6

Conditions	Yield
With sodium carbonate In water at 20℃; for 11h; Reagent/catalyst; Solvent; Large scale;	90.2%

7β-<(2R)-2-phenyl-2-amino>acetylamino-3-(1-methyl-1H-tetrazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid (73910-33-5) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → 7β-<(2R)-2-phenyl-2-(4-ethyl-2,3-dioxopiperazin-1-yl-carbonyl)amino>acetylamino-3-(1-methyl-1H-tetrazol-5-yl)thiomethyl-1-carba-1-dethia-3-cephem-4-carboxylic acid (73910-34-6)

Conditions	Yield
With benzenesulfonamide; methyloxirane In acetonitrile for 0.416667h;	90%

1-Ethyl-4-trimethylsilanyl-piperazine-2,3-dione + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → N,N'-carbonyl-bis-(4-ethyl-2,3-dioxopiperazine)

Conditions	Yield
In dichloromethane at -5 - 25℃; for 8.67h; Solvent;	84%

D-4-hydroxyphenylglycine (22818-40-2) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (R)-<<(4-ethyl-2,3-dioxo-1-piperazinyl)carbonyl>amino>(4-hydroxyphenyl)acetic acid (62893-24-7)

Conditions	Yield
With sodium carbonate; zinc dibromide In water at 200℃; for 3h; Temperature; Reagent/catalyst; Autoclave;	83.5%

α-amino-α-(2-benzyloxycarbonylaminothiazol-4-yl)acetic acid (72699-69-5) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (+/-)-α-(2-benzyloxycarbonylaminothiazol-4-yl)-α-(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)acetic acid (85208-16-8)

Conditions	Yield
With triethylamine In acetone for 1h; Ambient temperature;	69%

<4S,5R,6S(R)>-3-(hydroxymethyl)-6-<1-<(tert-butyldimethylsilyl)oxy>ethyl>-7-oxo-4-thia-1-azabicyclo<3.2.0>hept-2-enecarboxylic acid 2-allyl ester (88585-78-8) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (5R,6S)-6-[(R)-1-(tert-Butyl-dimethyl-silanyloxy)-ethyl]-3-(4-ethyl-2,3-dioxo-piperazine-1-carbonyloxymethyl)-7-oxo-4-thia-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid allyl ester

Conditions	Yield
With N,N-diethyl-N-isopropylamine In dichloromethane	51%

levodopa (59-92-7) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (S)-3-(3,4-Dihydroxy-phenyl)-2-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-propionic acid (263154-16-1)

Conditions	Yield
Stage #1: levodopa With chloro-trimethyl-silane; 1,1,1,3,3,3-hexamethyl-disilazane for 2h; silylation; Heating; Stage #2: 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride In dichloromethane at 20℃; for 1.5h; Acylation; Stage #3: With water In acetone for 0.3h; pH=1 - 2; desilylation;	49%

C18H19N7O5S2 + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → cefoperazone (62893-19-0, 68779-10-2)

Conditions	Yield
With potassium carbonate In water; ethyl acetate at 20℃;	42%

D-3,4-Dihydroxyphenyl glycine + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → D-2-[(4-Ethyl-2,3-dioxopiperazin-1-yl)carbonylamino]-2-(3,4-dihydroxyphenyl)acetic acid (74985-17-4)

Conditions	Yield
With chloro-trimethyl-silane In dichloromethane; water; acetone; 1,1,1,3,3,3-hexamethyl-disilazane	40%
With hydrogenchloride In diethyl ether; dichloromethane; ethyl acetate; acetone; N,N-diethyl-1,1,1-trimethylsilanamine	27%

2-(3-{[5-(2-aminoethoxy)benzothiazol-2-ylmethyl]amino}-[1,2,4]triazin-5-yl)-3-methylphenol hydrochloride + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → C27H28N8O5S (1426097-00-8)

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 0℃; Inert atmosphere;	29%

t-butyl 7β-(D-2-amino-2-phenylacetamido)-7α-formamidocephalosporanate + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → t-Butyl 7β-[D-2-[(4-Ethyl-2,3-dioxopiperazin-1-yl)carbonylamino]-2-phenylacetamido]-7α-formamidocephalosporanate

Conditions	Yield
With pyridine In dichloromethane	22%

4-(aminomethyl)-N-(2-nitro-5-(thiophen-2-yl)phenyl)benzamide hydrochloride (1364569-65-2) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → 4-ethyl-N-(4-(2-nitro-5-(thiophen-2-yl)phenylcarbamoyl)benzyl)-2,3-dioxopiperazine-1-carboxamide (1364569-75-4)

Conditions	Yield
With triethylamine In dichloromethane; N,N-dimethyl-formamide at 20℃;	22%

6-<(+/-)-α-amino-α-(2-aminothiazol-4-yl)acetamido>penicillanic acid (85208-10-2) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → 6-<(+/-)-α-(2-aminothiazol-4-yl)-α-(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)acetamido>penicillanic acid (85208-19-1, 85208-20-4, 85280-44-0) + 1-ethyl-2,3-dioxo-piperazine (59702-31-7)

Conditions	Yield
With sodium hydrogencarbonate 1.) THF, H2O, 0 deg C, 2.) pH=7-7.5, room temperature, 1 h;	A 21% B n/a

(4R,8S)-8-(E)-2-amino-1-(((tert-butyldimethylsilyl)oxy)imino)ethyl-5-(benzyloxy)-1-methyl-1,4,5,8-tetrahydro-6H-4,7-methanopyrazolo[3,4-e][1,3]diazepin-6-one + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → N-((E)-2-((4R,8S)-5-(benzyloxy)-1-methyl-6-oxo-4,5,6,8-tetrahydro-1H-4,7-methanopyrazolo[3,4-e][1,3]diazepin-8-yl)-2-(((tert-butyldimethylsilyl)oxy)imino)ethyl)-4-ethyl-2,3-dioxopiperazine-1-carboxamide

Conditions	Yield
With pyridine; triethylamine at 20℃; for 0.333333h;	18.4%

7β-<(2R)-2-phenyl-2-amino>acetylamino-3-methoxy-1-carba-1-dethia-3-cephem-4-carboxylic acid (73910-42-6) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → 7β-<(2R)-2-phenyl-2-(4-ethyl-2,3-dioxopiperazin-1-yl-carbonyl)amino>acetylamino-3-methoxy-1-carba-1-dethia-3-cephem-4-carboxylic acid (73910-43-7)

Conditions	Yield
With benzenesulfonamide; methyloxirane In acetonitrile	15 mg

CL191,121 (161855-50-1) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (4R,5S,6S)-3-((2R,3R)-2-{[(4-Ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-methyl}-tetrahydro-furan-3-ylsulfanyl)-6-((R)-1-hydroxy-ethyl)-4-methyl-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In dichloromethane

(4R,5S,6S)-3-(5-Aminomethyl-tetrahydro-furan-3-ylsulfanyl)-6-((R)-1-hydroxy-ethyl)-4-methyl-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → Sodium; (4R,5S,6S)-3-(5-{[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-methyl}-tetrahydro-furan-3-ylsulfanyl)-6-((R)-1-hydroxy-ethyl)-4-methyl-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylate

Conditions	Yield
With N-ethyl-N,N-diisopropylamine In dichloromethane

α-amino(3,4-dihydroxyphenyl)acetic acid hydrobromide + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → D-2-[(4-Ethyl-2,3-dioxopiperazin-1-yl)carbonylamino]-2-(3,4-dihydroxyphenyl)acetic acid (74985-17-4)

Conditions	Yield
Stage #1: α-amino(3,4-dihydroxyphenyl)acetic acid hydrobromide With chloro-trimethyl-silane; 1,1,1,3,3,3-hexamethyl-disilazane for 2h; silylation; Heating; Stage #2: 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride In dichloromethane at 20℃; for 1.5h; Acylation; Stage #3: With water In acetone for 0.3h; pH=1 - 2; desilylation;

D-Dopa (5796-17-8) + 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (R)-3-(3,4-Dihydroxy-phenyl)-2-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-propionic acid

Conditions	Yield
Stage #1: D-Dopa With chloro-trimethyl-silane; 1,1,1,3,3,3-hexamethyl-disilazane for 2h; silylation; Heating; Stage #2: 4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride In dichloromethane at 20℃; for 1.5h; Acylation; Stage #3: With water In acetone for 0.3h; pH=1 - 2; desilylation;

4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (3,4-dihydroxy-phenyl)-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-acetic acid 2,5-dioxo-pyrrolidin-1-yl ester

Conditions	Yield
Multi-step reaction with 2 steps 1.1: 1,1,1,3,3,3-hexamethyldisilazane; trimethylsilyl chloride / 2 h / Heating 1.2: CH2Cl2 / 1.5 h / 20 °C 1.3: water / acetone / 0.3 h / pH 1 - 2 2.1: DCC / tetrahydrofuran / 2 h View Scheme

4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (R)-3-(3,4-Dihydroxy-phenyl)-2-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-propionic acid 2,5-dioxo-pyrrolidin-1-yl ester

Conditions	Yield
Multi-step reaction with 2 steps 1.1: 1,1,1,3,3,3-hexamethyldisilazane; trimethylsilyl chloride / 2 h / Heating 1.2: CH2Cl2 / 1.5 h / 20 °C 1.3: water / acetone / 0.3 h / pH 1 - 2 2.1: DCC / tetrahydrofuran / 2 h View Scheme

4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (S)-3-(3,4-Dihydroxy-phenyl)-2-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-propionic acid 2,5-dioxo-pyrrolidin-1-yl ester

Conditions	Yield
Multi-step reaction with 2 steps 1.1: 1,1,1,3,3,3-hexamethyldisilazane; trimethylsilyl chloride / 2 h / Heating 1.2: CH2Cl2 / 1.5 h / 20 °C 1.3: 49 percent / water / acetone / 0.3 h / pH 1 - 2 2.1: DCC / tetrahydrofuran / 2 h View Scheme

4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (2S,3S)-3-{2-(3,4-Dihydroxy-phenyl)-2-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-acetylamino}-2-methyl-4-oxo-azetidine-1-sulfonic acid; compound with triethyl-amine

Conditions	Yield
Multi-step reaction with 3 steps 1.1: 1,1,1,3,3,3-hexamethyldisilazane; trimethylsilyl chloride / 2 h / Heating 1.2: CH2Cl2 / 1.5 h / 20 °C 1.3: water / acetone / 0.3 h / pH 1 - 2 2.1: DCC / tetrahydrofuran / 2 h 3.1: 61 mg / tetrahydrofuran; H2O / 3 h / 20 °C View Scheme

4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (2S,3S)-3-{(S)-3-(3,4-Dihydroxy-phenyl)-2-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-propionylamino}-2-methyl-4-oxo-azetidine-1-sulfonic acid; compound with triethyl-amine

Conditions	Yield
Multi-step reaction with 3 steps 1.1: 1,1,1,3,3,3-hexamethyldisilazane; trimethylsilyl chloride / 2 h / Heating 1.2: CH2Cl2 / 1.5 h / 20 °C 1.3: 49 percent / water / acetone / 0.3 h / pH 1 - 2 2.1: DCC / tetrahydrofuran / 2 h 3.1: 84 percent / tetrahydrofuran; H2O / 3 h / 20 °C View Scheme

4-ethyl-2,3-dioxopiperazine-1-carbonyl chloride (59703-00-3) → (2S,3S)-3-{(R)-3-(3,4-Dihydroxy-phenyl)-2-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-propionylamino}-2-methyl-4-oxo-azetidine-1-sulfonic acid; compound with triethyl-amine

Conditions	Yield
Multi-step reaction with 3 steps 1.1: 1,1,1,3,3,3-hexamethyldisilazane; trimethylsilyl chloride / 2 h / Heating 1.2: CH2Cl2 / 1.5 h / 20 °C 1.3: water / acetone / 0.3 h / pH 1 - 2 2.1: DCC / tetrahydrofuran / 2 h 3.1: 129 mg / tetrahydrofuran; H2O / 3 h / 20 °C View Scheme

Upstream product

• 149-30-4 2-Mercaptobenzothiazole 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 59702-31-7 1-ethyl-2,3-dioxo-piperazine 
• 75-44-5 phosgene 

Downstream Products

• 263154-16-1 (S)-3-(3,4-Dihydroxy-phenyl)-2-[(4-ethyl-2,3-dioxo-piperazine-1-carbonyl)-amino]-propionic acid 
• 62893-24-7 (R)-<<(4-ethyl-2,3-dioxo-1-piperazinyl)carbonyl>amino>(4-hydroxyphenyl)acetic acid 
• 85208-16-8 (+/-)-α-(2-benzyloxycarbonylaminothiazol-4-yl)-α-(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)acetic acid 
• 61477-96-1 piperacillin 
• 62893-19-0 cefoperazone 
• 1426097-00-8 C₂₇H₂₈N₈O₅S 
• 1364569-75-4 4-ethyl-N-(4-(2-nitro-5-(thiophen-2-yl)phenylcarbamoyl)benzyl)-2,3-dioxopiperazine-1-carboxamide 
• 74985-17-4 D-2-[(4-Ethyl-2,3-dioxopiperazin-1-yl)carbonylamino]-2-(3,4-dihydroxyphenyl)acetic acid 

Relevant articles and documents

Preparation method of piperacillin

The invention discloses a preparation method of piperacillin. According to the method, DBU with stronger alkalinity is used as an initiator to promote the reaction of N-ethyl-2, 3-dioxopiperazine andtriphosgene to obtain N-ethyl-2, 3-dioxopiperazine acyl chloride, so that the use of trimethylchlorosilane is avoided; In the condensation reaction, sodium acetate is used as an acid-binding agent, sothat the pollution of carbon dioxide to the environment is avoided. The alkalinity of sodium acetate is weaker than that of sodium bicarbonate, the hydrolysis degree in the reaction process is low, meanwhile, DBU is used as a catalyst, and the N-ethyl-2, 3-dioxopiperazine acyl chloride hydrolysate can also react with ampicillin to obtain piperacillin, so that the reaction yield is increased, andthe production cost is further reduced.

A method for preparing paipai pulls the xilin acid (by machine translation)

The invention discloses a method for preparing paipai pulls the xilin acid. The invention is directed to preparation method in the prior existing "N - ethyl hydrogen peroxide piperazine conversion is relatively low, a condensation step the non-condensable gas carbon dioxide, solvent loss is relatively large" disadvantages, this invention adopts the pyridine in place of the triethylamine as acid, in the acylation reaction of adding triphosgene is added a catalytic amount of 4 - dimethyl amino pyridine as an initiator, can effectively improve the reaction activity of the triphosgene, so that the N - ethyl hydrogen peroxide piperazine acyl chloride conversion is improved by about 10%. The invention in the condensation reaction, binary weak alkali such as for calcium carbonate to replace the one dollar weak alkali sodium bicarbonate, help to reduce the degradation, condensation reaction yield is improved by about 5%, at the same time can reduce the generation of carbon dioxide gas causes non-condensable 50%. (by machine translation)

Novel penicillins and cephalosporins and process for producing the same

Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.