144034-80-0 Usage
Uses
Different sources of media describe the Uses of 144034-80-0 differently. You can refer to the following data:
1. Rizatriptan is reported to be a very effective acute migraine drug. It is reported to display high agonist activity at mainly the serotonin 5-HT1B and 5-HT1D receptor subtypes.
2. Ca channel blocker
Brand name
Maxalt (Merck).
General Description
Rizatriptan, approved in 1998, is a fast-acting triptan becauseof its moderate lipophilicity yet has a very shortelimination half-life similar to sumatriptan (i.e., like sumatriptan,it is mainly metabolized by MAO-A). The only advantagesof this drug when compared with sumatriptan arethat it has a slightly faster onset and that it has an orallydisintegrating tablet formulation which can be taken withoutwater.
Drug interactions
Potentially hazardous interactions with other drugs
Antidepressants: increased risk of CNS excitation
with citalopram - avoid; risk of CNS toxicity
with MAOIs, moclobemide and linezolid - avoid
for 2 weeks after discontinuation of MAOI and
moclobemide; possibly increased serotonergic
effects with duloxetine and venlafaxine; increased
serotonergic effects with St John’s wort - avoid.
Dapoxetine: possible increased risk of serotonergic
effects - avoid for 2 weeks after stopping 5HT1
agonists.
Ergot alkaloids: increased risk of vasospasm - avoid.
Propranolol: rizatriptan levels increased, reduce dose
of rizatriptan to 5 mg (max 10 mg in 24 hours).
Metabolism
The main route of rizatriptan metabolism is via oxidative
deamination by monoamine oxidase-A (MAO-A)
to the indole acetic acid metabolite, which is not
pharmacologically active. N-monodesmethyl-rizatriptan,
a metabolite with activity similar to that of parent
compound, is formed to a minor degree, but does not
contribute significantly to the pharmacodynamic activity
of rizatriptan.
Less than 1% is excreted in the urine as active
N-monodesmethyl metabolite.
Check Digit Verification of cas no
The CAS Registry Mumber 144034-80-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,4,4,0,3 and 4 respectively; the second part has 2 digits, 8 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 144034-80:
(8*1)+(7*4)+(6*4)+(5*0)+(4*3)+(3*4)+(2*8)+(1*0)=100
100 % 10 = 0
So 144034-80-0 is a valid CAS Registry Number.
InChI:InChI=1/C15H19N5.C7H6O2/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20;8-7(9)6-4-2-1-3-5-6/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3;1-5H,(H,8,9)
144034-80-0Relevant articles and documents
A novel and convenient route for the construction of 5-((1H-1,2,4-triazol- 1-yl)methyl)-1H-indoles and its application in the synthesis of Rizatriptan
He, Yi,Li, Xiaolong,Li, Jue,Li, Xiaocen,Guo, Li,Hai, Li,Wu, Yong
, p. 3938 - 3941 (2014)
In this study, a novel and convenient route for the construction of 5-((1H-1,2,4-triazol-1-yl)methyl)-1H-indoles (8) is presented starting from (1H-1,2,4-triazol-1-yl)methanol (5) and indolines (6) under 98% H 2SO4 at room temperature for 4-24 h, followed by deacetylation and dehydrogenation. Based on this finding, a novel route to synthesize Rizatriptan starting from tryptamine was designed and accomplished with 48.5% overall yield in 6 steps. Compared with operational art, the new route afforded higher yield and more pure products requiring no chromatographic purification, which may further be applied in industrialization.
Rizatriptan preparation method
-
, (2018/09/08)
The invention discloses a rizatriptan preparation method, wherein 5-methyltryptamine is used as a raw material, and five steps of amino methylation, bromination, Boc amino protection, triazole substitution and Boc deprotection are performed to obtain rizatriptan. According to the present invention, the existing indole synthesis method is avoided by using 5-methyltryptamine as the starting raw material, the used reagent is environmentally friendly, and the preparation method has characteristics of simpleness, mild condition and simple post-treatment, is suitable for industrial promotion, and isthe completely-new rizatriptan preparation method.
Method for preparing the advantage grips Qu Tan a benzoic acid
-
Paragraph 0041-0043, (2017/02/09)
The invention discloses a novel preparation method for rizatriptan benzoate. The preparation method uses indoline as a starting material, and performs five-step reaction of triazole methylation, dehydrogenation, side chain formation, reduction and salt formation so as to obtain the rizatriptan benzoate. The innovative point of the method is that a brand-new method for forming an indole ring is adopted, and the defects caused by a fisher indole synthesis method adopted in a conventional course that the impurity content of the product is high, and the purification is difficult. The method has the advantages that the operation is simple and convenient, the reaction condition is mild, no expensive reagent is used, and the product purity is high.
