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Paliperidone Palmitate

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Paliperidone Palmitate Basic information

Product Name:
Paliperidone Palmitate
Synonyms:
  • (9RS)-3-(2-(4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl)et hyl)-2-Methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2-a)pyriMi din-9-yl hexadecanoate
  • Hexadecanoic acid 3-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl]-ethyl]-6,7,8,9-tetrahydro-2-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl ester
  • Paliperidone Palmitate
  • Paliperidone Palmitate [USAN]
  • Invega Sustenna
  • RO 92670
  • 9-Hydroxyrisperidone palmitate
  • Hexadecanoic acid 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl ester
CAS:
199739-10-1
MF:
C39H57FN4O4
MW:
664.89
EINECS:
225-799-5
Product Categories:
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • API
Mol File:
199739-10-1.mol
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Paliperidone Palmitate Chemical Properties

Melting point:
110-115°C
Boiling point:
736.3±70.0 °C(Predicted)
Density 
1.19
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
Chloroform (Slightly), Ethyl Acetate (Slightly, Heated, Sonicated), Methanol (Slightly)
form 
Solid
pka
8.07±0.10(Predicted)
color 
Off-White to Light Beige
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Paliperidone Palmitate Usage And Synthesis

Description

Paliperidone palmitate is an atypical long acting antipsychotics,which can fast onset in acute phase and continuously improve the symptoms in maintenance phase. It has the solid efficacy and convenient ad[1]ministration,which offer a new option for schizophrenia treatment and will help patients to adhere the treatment and prevent relapse. As the sole long acting antipsychotics with monthly injection,it was approved by CFDA in 2011 and indicated for the acute and maintenance treatment of schizophrenia.

Uses

Paliperidone Palmitate is a long-acting injectable atypical antipsychotic used in the treatment of schizophrenia.

Definition

ChEBI: 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl hexadecanoate is a fatty acid ester obtained by the formal condensation of the carboxy group of hexadecanoic acid with the hydroxy group of 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one. It is a member of 1,2-benzoxazoles, a heteroarylpiperidine, an organofluorine compound, a pyridopyrimidine and a fatty acid ester.

Side effects

The review of the literature also underlined that paliperidone palmitate is well tolerated, compared with placebo. Frequency and severity of side-effects such as extrapyramidal symptoms, hyperprolactinemia and weight gain, was similar or less than those found in treatment with other atypical antipsychotics, including long-acting ones.

Paliperidone PalmitateSupplier

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