Novel guanidine mimics as factor Xa inhibitors
An atomistic, compound-based technique applied in the field of novel guanidine mimetics as factor Xa inhibitors, able to resolve unspecified issues, etc.
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[0217] Scheme 6 illustrates the preparation method of aminobenzimidazole aldehyde, which can be joined to a C-linked or N-linked heterocyclic ring according to the method described in the synthesis section later. Cyclization of 3,4-diaminobenzoate gives cbz-protected 2-aminobenzimidazole, followed by DIBAL reduction and oxidation to give the desired aldehyde.
[0218] Process 6
[0219] Scheme 7 describes the preparation method of N-linked aminobenzisoxazole, aminoindazole, diaminoquinazoline and aminoquinazoline of formula I. At room temperature to the reflux temperature of the selected solvent, in protic or aprotic solvents (with or without miscible co-solvents), use stannous chloride or other suitable reducing agents, commercially available The aniline derivatives prepared from 2-fluoro-5-nitrobenzonitrile can be used to prepare this type of compound.
[0220] According to the foregoing, N-linked 3-aminobenzisoxazole and 3-aminoindazole can be obtained. By...
Embodiment 1
[0354] Example 11-(1'-Amino-isoquinolin-7'-yl)-3-methyl-5-[(2'-aminosulfonyl-[1,1']-biphenyl-4-yl)
[0355] Carbonylamino]pyrazole, methanesulfonate
[0356] At 0°C, 7-aminoisoquinine (6.26 g, 43.4 mmol) (J. Chem. Soc. 1951, 2851) was added to 40 ml of concentrated hydrochloric acid. Sodium nitrite (3.0g, 43.4mmol) was dissolved in 15ml of water, cooled to 0°C and added dropwise to the above isoquinine solution. The reaction was stirred at 0°C for 30 minutes. Dissolve stannous chloride dihydrate (29.3g, 130.2mmol, 3eq) in 25ml of concentrated hydrochloric acid, cool the solution to 0°C, and add dropwise to the above isoquinine solution. The reaction was placed in the refrigerator overnight. The precipitate was separated by filtration the next day, washed with 100 ml of ice-cold brine, followed by 100 ml of a 2:1 petroleum ether / diethyl ether solution. The brown solid was dried under dynamic vacuum overnight. The tin double salt of isoqui...
Embodiment 21
[0361] Example 21-(1'-Amino-isoquinolin-7'-yl)-3-methyl-5-[(2'-methanesulfonyl-[1,1']-biphenyl-4-yl) carbonyl
[0362] Amino]pyrazole methanesulfonate
[0363] According to a method similar to that described in Example 1, the target compound was prepared. MS(ES+): 498.0(M+H) + (100%), mp 175°C.
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