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2020年6月20日星期六

Intermediates of Relugolix

FDA New, GMP Do
Clinical Phase II, III Intermediates
GMP Custom synthesis, Full Document

R&D Center: 8000 sq, More than 100 hoods
Pilot Plant: 20000sq, 40 reactors from 5-200L
Manufacturing Site: 800000sq, 40 reactors from 100-5000L



Intermediates of Relugolix, 4-(N-benzyl-N-methylaminomethyl)-2-[N-(2,6-difluorobenzyl)-N-ethoxycarbonylamino]-5-[4-(3-methoxyureido)phenyl]thiophene-3-carboxylic acid, CAS 308831-99-4, stock 11.5kg, assay 98.4%.

Intermediates of Relugolix, Ethyl 2-[(2,6-difluorobenzyl)(ethoxycarbonyl)amino]-4-{[(2-methoxyethyl)(methyl)amino]methyl}-5-(4-nitrophenyl)thiophene-3-carboxylate, CAS 308832-01-1, stock 32.9kg, assay 99.3%.

Intermediates of Relugolix, ethyl 5-(4-aminophenyl)-2-[(2,6-difluorobenzyl)(ethoxycarbonyl)amino]-4-{[(2-methoxyethyl)(methyl)amino]methyl}thiophene-3-carboxylate, CAS 577780-07-5, stock 10.6kg, assay 98.8%.

Intermediates of Relugolix, ethyl 2-[(2,6-difluorobenzyl)(ethoxycarbonyl)amino]-5-{4-[(methoxycarbamoyl)amino]phenyl}-4-{[(2-methoxyethyl)(methyl)amino]methyl}thiophene-3-carboxylate, CAS 737789-92-3, stock 10.3kg, assay 99.5%.

Intermediates of Relugolix, Ethyl 4-(bromomethyl)-2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-5-(4-nitrophenyl)thiophene-3-carboxylate, CAS 308831-95-0, stock 20kg, assay 98.3%.

Intermediates of Relugolix, 1-(4-(5-((benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea, CAS 737789-81-0, stock 17.1kg, assay 98%.

Intermediates of Relugolix, 1-(4-(1-(2,6-difluorobenzyl)-3-(6-methoxypyridazin-3-yl)-5-((methylamino)methyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea, CAS 737790-54-4, stock 9.7kg, assay 98.2%.

Intermediates of Relugolix, 2-((2,6-difluorobenzyl)(ethoxycarbonyl)amino)-4-(((2-methoxyethyl)(methyl)amino)methyl)-5-(4-(3-methoxyureido)phenyl)thiophene-3-carboxylic acid, CAS 737789-93-4, stock 7.3kg, assay 98.7%.

Intermediates of Relugolix, 1-(4-(1-(2,6-difluorobenzyl)-5-(((2-methoxyethyl)(methyl)amino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea, CAS 737789-61-6, stock 9.3kg, assay 98.7%.

Intermediates of Relugolix, 1-(4-(5-(chloromethyl)-1-(2,6-difluorobenzyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea, CAS 737790-51-1, stock 21.7kg, assay 98.4%.