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18162-48-6872-50-4Methylene ChloridenaphthaleneTHFTitanium Dioxide
ChemicalBook CAS DataBase List Tadalafil
171596-29-5

Tadalafil synthesis

6synthesis methods
D-(-)-Tryptophan methyl ester (175) and 1,3- benzodioxole-5-carboxaldehyde (176) were subjected to a modified Pictet-Spengler reaction to form cis- and transtetrahydro- β-carboline tricyclic compounds. The ciscompound 177 was isolated as a white solid in 42% yield. The basic nitrogen in the piperidine ring of 177 was acylated with chloroacetyl chloride (179) to give compound 180 in 93% yield. Finally, the diketonepiperazine ring was formed by adding 180 to 33% methylamine in ethanol under refluxing conditions and yielded tadalafil (XXII) in 77% as a white solid.

74-89-5 Synthesis
Methylamine

74-89-5
0 suppliers
$13.44/25ML

171489-59-1 Synthesis
Chloropretadalafil

171489-59-1
304 suppliers
$7.00/1g

Tadalafil

171596-29-5
1002 suppliers
$10.00/1g

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Yield:171596-29-5 95.3%

Reaction Conditions:

in methanol; for 3 h;Reflux;Large scale;

Steps:

20-21 Synthesis of Tadalafil

Add Intermediate 3 (20kg, 47mol), 30% methylamine methanol solution (25kg, 235mol), 140L of methanol was added to the reactor, Heat and stir to reflux, keep the reaction for 3h, After the reaction was detected by HPLC, it was cooled down to room temperature, centrifuged and washed with a small amount of methanol. The product was dried to obtain 17.3 kg of a white solid with a yield of 95.3% and a purity of 99.3%.

References:

CN110437228,2019,A Location in patent:Paragraph 0083-0088

120-57-0 Synthesis
Piperonyl aldehyde

120-57-0
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$26.36/25g

2,5-Piperazinedione, 3-(1H-indol-3-ylmethyl)-1-methyl-, (3R)-

1422164-53-1
8 suppliers
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Tadalafil

171596-29-5
1002 suppliers
$10.00/1g

References
Tadalafil iMpurity B

951661-82-8
33 suppliers
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79-04-9 Synthesis
Chloroacetyl chloride

79-04-9
374 suppliers
$12.00/5g

Tadalafil

171596-29-5
1002 suppliers
$10.00/1g

References
171489-59-1 Synthesis
Chloropretadalafil

171489-59-1
304 suppliers
$7.00/1g

Tadalafil

171596-29-5
1002 suppliers
$10.00/1g

References
1H-Pyrido[3,4-b]indole-3-carboxylic acid, 1-(1,3-benzodioxol-5-yl)-2-[[[(9H-fluoren-9-ylmethoxy)carbonyl]methylamino]acetyl]-2,3,4,9-tetrahydro-, methyl ester, (1R,3R)- (9CI)

749864-18-4
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Tadalafil

171596-29-5
1002 suppliers
$10.00/1g

References

Tadalafil Related Search:

Potassium hydride Hydrocortisone Methylparaben Methyl acetate Methyl salicylate L-Tryptophan D-Tryptophan (1S,3S)-1-(1,3-Benzodioxol-5-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic Acid Methyl Ester cis-Tadalafil Taladafil impurity