CAS 2905-62-6

3,5-Dichloro-1-benzenecarbonyl chloride3,5-dichlorobenzoyl chloride

Codes: (I)409139-3-a, (I)409139-4-a, TAFA-002, (II)409139-1-a

Application context (from source-drug indications)

Transthyretin amyloidosisTafamidisHeart diseaseTafamidisAmyloid polyneuropathyTafamidis MeglumineTransthyretin amyloidosisTafamidis MeglumineAmyloidosisTafamidis MeglumineCardiomyopathyTafamidis MeglumineLight-chain (AL) amyloidosisTafamidis MeglumineFamilial amyloid neuropathyTafamidis Meglumine

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Tafamidis	Tier C — Watch / trade	-
Tafamidis Meglumine	Tier B — Position early	-

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

TafamidisOptimised routesteps: 4total yield: /

3,5-Dichloro-1-benzenecarbonyl chloride→3,5-Dichloro-N-methyl-N-phenylbenzamide→N-[(3,5-Dichlorophenyl)(methoxy)methylidene]-N-methylbenzeniminium trifluoromethanesulfonate→1,3-Dichloro-5-(trimethoxymethyl)benzene→2-(Hydroxymethyl)-2-phenylpropane-1,3-diol→2-Phenylacetaldehyde→2-Ethyl-2-(hydroxymethyl)propane-1,3-diol→1-(3,5-Dichlorophenyl)-4-phenyl-2,6,7-trioxabicyclo[2.2.2]octane→1-(3,5-Dichlorophenyl)-4-ethyl-2,6,7-trioxabicyclo[2.2.2]octane→(4-Carboxy-2-hydroxyphenyl)amine→2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid

TafamidisOptimised routesteps: 3total yield: /

3,5-Dichloro-1-benzenecarbonyl chloride→(3-Methyloxetan-3-yl)methanol→(3-Methyloxetan-3-yl)methyl 3,5-dichlorobenzoate→1-(3,5-Dichlorophenyl)-4-methyl-2,6,7-trioxabicyclo[2.2.2]octane→(4-Carboxy-2-hydroxyphenyl)amine→2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid

Tafamidis MeglumineOriginator routesteps: 5total yield: 3.35 g

4-amino-3-hydroxybenzoic acid→3,5-dichlorobenzoyl chloride→4-(3,5-dichlorobenzamido)-3-hydroxybenzoic acid→2-(3,5-dichlorophenyl)benzo[d]oxazole-6-carboxylic acid→methyl 2-(3,5-dichlorophenyl)benzo[d]oxazole-6-carboxylate

Tafamidis MeglumineOptimised routesteps: 7total yield: /

3,5-Dichlorobenzoic acid→3,5-Dichloro-1-benzenecarbonyl chloride→(4-Carboxy-2-hydroxyphenyl)amine→2-Bromo-4-methoxycarbonylaniline→2-Hydroxy-4-methoxycarbonylaniline→4-Amino-3-hydroxybenzoic acid methyl ester hydrochloride→4-(3,5-Dichlorobenzamido)-3-hydroxybenzoic acid→Methyl 3-bromo-4-(3,5-dichlorobenzamido)benzoate→Methyl 4-(3,5-dichlorobenzamido)-3-hydroxybenzoate→2-(3,5-Dichlorophenyl)benzoxazole-6-carboxylic acid methyl ester→Methyl 1,3-benzoxazole-6-carboxylate→1,3-Bis(chloranyl)benzene→2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid→3-Carboxyphenol→3-Carboxy-6-nitrophenol

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