- CYCLIC AMINE COMPOUND
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A compound represented by the formula (I) or a salt thereof: (I) wherein the ring A represents a 5- to 8-membered ring which may have additional substituent besides R6, R7 and R8; R1 represents an electron-attracting group; R2, R3, R4 and R5 independently represent a hydrogen atom, a halogen atom, a group attached through a carbon atom, a group attached through a nitrogen atom, a group attached through an oxygen group, or a group attached through a sulfur atom; R6 represents a halogen atom, a group attached through a carbon atom, a group attached through a nitrogen atom, a group attached through an oxygen group, or a group attached through a sulfur atom, and R7 represents a cyano group, a nitro group, an acyl group which may have a substituent, a carboxyl group which may be esterified or amidated, or a hydrocarbon group which may have a substituent, or R6 and R7 together with a carbon atom to which they are attached may form a ring which may have a substituent; and R8 represents a hydrogen atom, a halogen atom, a group attached through a carbon atom, a group attached through an oxygen atom, or a group attached through a sulfur atom. The compound or salt has an excellent androgen receptor modulating effect, and is useful for the prevention/treatment of hypogonadism, partial androgen deficiency in aging male, decline in physical strength, cachexia, osteoporosis and the like.
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Page/Page column 114-115
(2010/11/25)
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- Process for preparing fluorobenzonitriles
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Fluorobenzonitriles and chlorofluorobenzonitriles are prepared in an advantageous manner from the corresponding chlorobenzonitriles and an alkali metal fluoride in a chlorine-fluorine exchange reaction, by catalyzing the reaction with a quaternary ammonium compound comprising at least one alkoxypolyoxyalkyl radical.
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- Processes for producing 5-fluorobenzoic acids and their intermediates
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A process for producing a 5-fluorobenzoic acid of the formula (V), which comprises trichloromethylating a fluorobenzene of the formula (I) to obtain a 5-fluorobenzotrichloride of the formula (II), then reacting it with aqueous ammonia to obtain a 5-fluorobenzonitrile of the formula (III), reacting it with a fluorinating agent to obtain a 5-fluorobenzonitrile of the formula (IV) and hydrolyzing it: STR1 wherein each of X1, X3, Y1 and Y3 is a halogen atom, and each of X2 and Y2 is hydrogen or a halogen atom.
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