Ritipenemacoxil

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Names

[ Name ]:
Ritipenemacoxil

[Synonym ]:
Ritanserinum [Latin]
Ritanserine
Ritanserinum
Ritanserine [French]
ritanserin
Ritanserina
risperidone
Acetoxymethyl(5R,6S)-2-carbamoyloxy-methyl-6-[1(R)hydroxyethyl]penem-3-carboxylate
Tiserton
Ritanserina [Spanish]

Chemical & Physical Properties

[ Density]:
1.57g/cm3

[ Boiling Point ]:
656ºC at 760 mmHg

[ Molecular Formula ]:
C₁₃H₁₆N₂O₈S

[ Molecular Weight ]:
360.34000

[ Flash Point ]:
350.6ºC

[ Exact Mass ]:
360.06300

[ PSA ]:
171.75000

[ Index of Refraction ]:
1.62

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XI0192000

CHEMICAL NAME :: 4-Thia-1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid, 3-(((aminocarbonyl)oxy)methyl)-6- (1-hydroxyethyl)-7-oxo-, (acetyloxy)methyl ester, (5R-(5-alpha,6-alpha(R*)))-

CAS REGISTRY NUMBER :: 87238-52-6

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C13-H16-N2-O8-S

MOLECULAR WEIGHT :: 360.37

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: JACHDX Journal of Antimicrobial Chemotherapy. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1975- Volume(issue)/page/year: 23(Suppl C),129,1989

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4363 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: JACHDX Journal of Antimicrobial Chemotherapy. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1975- Volume(issue)/page/year: 23(Suppl C),129,1989 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91 gm/kg/26W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - urine volume decreased Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Metabolism (Intermediary) - lipids including transport

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 23,34,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 42 gm/kg/2W-I

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: JACHDX Journal of Antimicrobial Chemotherapy. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1975- Volume(issue)/page/year: 23(Suppl C),129,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 73 gm/kg/26W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes Kidney, Ureter, Bladder - changes in bladder weight

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 23,34,1995

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

(5R,6S)-acetoxymethyl 3-((carbamoyloxy)methyl)-7-oxo-6-((R)-1-((trimethylsilyl)oxy)ethyl)-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
acetyloxymethyl 2-chloro-2-oxoacetate
acetoxymethyl oxalic acid
acetoxymethyl 2-((2R,3S)-2-((2-(carbamoyloxy)acetyl)thio)-4-oxo-3-((R)-1-((trimethylsilyl)oxy)ethyl)azetidin-1-yl)-2-oxoacetate