1138245-21-2

  • Product Name:Mirogabalin besylate
  • Molecular Formula:C18H25NO5S
  • Purity:99%
  • Molecular Weight:367.466
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Product Details:

CasNo: 1138245-21-2

Molecular Formula: C18H25NO5S

Buy High Quality Mirogabalin besylate 1138245-21-2 Competitive Price

  • Molecular Formula:C6H6O3S*C12H19NO2
  • Molecular Weight:367.466

Mirogabalin besylate(Cas 1138245-21-2) Usage

Description

Mirogabalin besylate belongs to the class of drugs known as gabapentinoids. It is formulated as film-coated tablets for oral administration.
Uses

Mirogabalin besylate is approved in Japan for the treatment of two types of neuropathic pain:

Postherpetic neuralgia: This condition refers to nerve pain that persists after a shingles (herpes zoster) outbreak has healed.
Painful diabetic peripheral neuropathy: This condition involves nerve damage due to diabetes, leading to pain in the extremities.

1138245-21-2 Relevant articles

Mirogabalin besylate in the treatment of neuropathic pain

Burgess, J.Javed, S.Frank, B.Malik, R. A.Alam, U.

Drugs of today: Medicamentos de actualidad, 2020

Mirogabalin has a potent pain-modulating effect with a unique high affinity and prolonged dissociation rate for the alpha(2)delta-1 subunit of voltage-gated calcium (Ca2+) channels (VGCCs) on the dorsal root ganglion resulting in more sustained analgesia compared with traditional gabapentinoids.

Clinical Effectiveness of Mirogabalin Besylate for Trigeminal Neuropathy after Skull Base Surgery: Illustrative Cases

K Karatsu,R Tamura,T Miyauchi,J Sogano,U Hino,T Iwama,M Toda

Page/Page column 52, (2010/06/17)

Mirogabalin besylate is a selective ligand for the α2δ subunit of voltage-gated calcium channels. Although mirogabalin has been used for patients with postherpetic neuralgia and painful diabetic peripheral neuropathy, few reports have assessed the effect on postsurgical neuropathy.

1138245-21-2 Process route

DS-5565
1138245-13-2

DS-5565

benzenesulfonic acid
98-11-3

benzenesulfonic acid

[(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate
1138245-21-2

[(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate

Conditions
Conditions Yield
In water; Heating;
77%
In tert-butyl methyl ether; water; acetone; at -10 - 20 ℃; for 4.5h; Reagent/catalyst; Solvent; Temperature; Time;
 
diethyl [(1R,5S)-3-ethylbicyclo[3.2.0]hept-3-en-6-ylidene]propanedioate

diethyl [(1R,5S)-3-ethylbicyclo[3.2.0]hept-3-en-6-ylidene]propanedioate

[(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate
1138245-21-2

[(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate

Conditions
Conditions Yield
Multi-step reaction with 4 steps
1.1: ethanol / 4 h / 20 °C
2.1: potassium hydroxide / ethanol; water / 10 h / 20 °C / Reflux
2.2: 10 - 20 °C
3.1: hydrogenchloride / water; tert-butyl methyl ether / 20 °C
3.3: sponge cobalt; dimethylpolysiloxane / 7.5 h / 40 °C / 3375.34 Torr
4.1: acetone; water; tert-butyl methyl ether / 4.5 h / -10 - 20 °C
With hydrogenchloride; potassium hydroxide; In ethanol; tert-butyl methyl ether; water; acetone;
 
Multi-step reaction with 4 steps
1.1: ethanol / 4 h / 20 °C
2.1: potassium hydroxide / ethanol / 7.5 h / Reflux
2.2: 2 h / 20 °C
2.3: 20 °C
3.1: hydrogenchloride / water; toluene
3.2: sponge nickel / 3 h / 20 °C / 3040.2 Torr
3.3: 0.5 h
4.1: acetone; water; tert-butyl methyl ether / 4.5 h / -10 - 20 °C
With hydrogenchloride; potassium hydroxide; In ethanol; tert-butyl methyl ether; water; acetone; toluene;
 
Multi-step reaction with 4 steps
1: ethanol / 4 h / 20 °C
2: potassium hydroxide / ethanol; water / 8 h / 26 - 27 °C / Reflux
3: ammonium hydroxide; hydrogen; potassium hydroxide / water / 15 h / 40 °C / 3000.3 Torr
4: acetone; water; tert-butyl methyl ether / 4.5 h / -10 - 20 °C
With ammonium hydroxide; hydrogen; potassium hydroxide; In ethanol; tert-butyl methyl ether; water; acetone;
 
Multi-step reaction with 5 steps
1.1: ethanol / 4 h / 20 °C
2.1: potassium hydroxide / ethanol; water / 8 h / 26 - 27 °C / Reflux
3.1: hydrogenchloride / toluene / 22 - 46 °C
4.1: hydrogenchloride / water; tert-butyl methyl ether / 20 °C
4.3: sponge cobalt; dimethylpolysiloxane / 7.5 h / 40 °C / 3375.34 Torr
5.1: acetone; water; tert-butyl methyl ether / 4.5 h / -10 - 20 °C
With hydrogenchloride; potassium hydroxide; In ethanol; tert-butyl methyl ether; water; acetone; toluene;
 
Multi-step reaction with 5 steps
1.1: ethanol / 4 h / 20 °C
2.1: potassium hydroxide / ethanol / 8 h / Reflux
2.2: 20 h / 20 °C
2.3: 20 °C
3.1: hydrogenchloride / water; toluene
4.1: ammonium hydroxide; hydrogen; potassium hydroxide / water / 15 h / 40 °C / 3000.3 Torr
5.1: acetone; water; tert-butyl methyl ether / 4.5 h / -10 - 20 °C
With hydrogenchloride; ammonium hydroxide; hydrogen; potassium hydroxide; In ethanol; tert-butyl methyl ether; water; acetone; toluene;
 
Multi-step reaction with 6 steps
1.1: ethanol / 4 h / 20 °C
2.1: potassium hydroxide / ethanol / 8 h / Reflux
2.2: 20 h / 20 °C
2.3: 20 °C
3.1: hydrogenchloride / water; toluene
4.1: hydrogenchloride / toluene / 22 - 46 °C
5.1: hydrogenchloride / water; tert-butyl methyl ether / 20 °C
5.3: sponge cobalt; dimethylpolysiloxane / 7.5 h / 40 °C / 3375.34 Torr
6.1: acetone; water; tert-butyl methyl ether / 4.5 h / -10 - 20 °C
With hydrogenchloride; potassium hydroxide; In ethanol; tert-butyl methyl ether; water; acetone; toluene;
 

1138245-21-2 Upstream products

  • 1138245-13-2
    1138245-13-2

    DS-5565

  • 98-11-3
    98-11-3

    benzenesulfonic acid

  • 1235479-61-4
    1235479-61-4

    (1R,5S)-3-ethylbicyclo[3.2.0]hept-3-en-6-one

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