KR870002140A - Method for preparing bicyclic compound - Google Patents

Abstract

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Description

Method for preparing bicyclic compound

Since this is an open matter, no full text was included.

Claims (10)

To prepare a compound of formula (I) wherein R ⁴ and R ^{5 together} are oxo, react the compound of formula (II) with a compound of formula (III): or R ¹ is alkanoyl or aroyl And R ² is alkyl, Y is -CH _2- , -CH ₂ CH ₂ -or -N (R ₆ )-and R ⁶ is alkyl or aralkyl, to prepare a compound of formula (I) Reacting a compound of formula (IV) with an alkali metal salt of a compound of formula (V): R ¹ is alkanoyl or aroyl, R ² is alkyl, R ⁴ , R ⁵ together are oxo and Y is -CH _2- Or to prepare a compound of formula (I) wherein -CH ₂ CH ₂ -is ring-closed: or R ¹ is alkanoyl or aroyl and R ² is alkyl and R ⁴ and To prepare a compound of formula (I) wherein R ⁵ is oxo and Y is —CH— or —CH ₂ CH ₂ —, the compound of formula (VII) is closed: R ¹ is alkanoyl or Aro And R ² is alkyl, R ⁴ and R ⁵ together are oxo and Y is -NH- in case you wish to prepare a compound of formula (I), ring closure to the compound of the formula (VIII) or: R ¹ is To prepare a compound of formula (I) wherein alkanoyl or aroyl, R ² is alkyl and R ⁴ and R ⁵ together are hydrogen, R ¹ is alkanoyl or aroyl and R ² is alkyl and R ⁴ and Reduce the compound of formula (I) wherein R ⁵ together is oxo: Formula (I) wherein R ¹ is alkanoyl or aroyl, Y is -N (R ⁶ )-and R ⁶ is alkyl or aralkyl To prepare a compound of, the compound of formula (I) wherein R ¹ is alkanoyl or aroyl and Y is -NH- is reacted with a compound of formula (IX) or R ¹ is hydrogen When preparing a compound of (I), a compound of formula (I) wherein R ¹ is alkanoyl or aroyl is treated with a base: or a compound of formula (I) wherein R ² is hydrogen To prepare a compound of formula (I) wherein R ² is alkyl is treated with an acid or a base: or R ¹ is alkanoyl or aroyl and Y is -CH _2- , -CH ₂ CH ₂ -or- When preparing a compound of formula (I) wherein N, R ⁶ -and R ⁶ is alkyl or aralkyl, the compounds of formula (I) wherein the corresponding R ¹ is hydrogen are suitably alkanoylated or Aroylation: if necessary, the mixture of the resulting diastereomeric racemates is isolated / solidified into diastereomeric racemates or optically pure diastereomers: if necessary, the obtained racemates Isolation by optically coarse: if necessary, a compound of formula (I), wherein R ² is hydrogen, is converted into a pharmaceutically acceptable salt with a base, or Y obtained with -N (R ⁶ )- Converting the compound of formula (I) to an pharmaceutically acceptable salt with an acid Characterized in that when the compound of formula (I) and R ² is hydrogen, its pharmaceutically acceptable salt as a base and, when Y is -N (R ⁶ )-, it is pharmaceutically Methods of preparing acceptable salts. Wherein R ¹ is hydrogen, alkanoyl or aroyl: R ² is hydrogen or alkyl: R ³ is hydrogen or aryl: R ⁴ and R ⁵ are each hydrogen or R ⁴ and R ⁵ together are oxo : Y is -CH _2- , -CH ₂ CH ₂ -or -N (R ⁶ )-: R ⁶ is hydrogen, alkyl or aralkyl: R ²⁰ is alkyl: Y ¹ is -CH ₂ -,- CH ₂ CH ₂ -or-N (R ⁶⁰ )-: R ⁶⁰ is alkyl or aralkyl: Z is a leaving group: R ¹⁰ is alkanoyl or aroyl: Y ² is -CH ₂ -or -CH ₂ CH _2- : Hal is halogen. The method of claim 1, wherein R ¹ is hydrogen. The method of claim 1 or 2, wherein R ² is hydrogen. The process of claim 1, wherein R ³ is hydrogen. The method of any one of claims 1-4, wherein Y is -CH _2- . The method of any one of claims 1-5, wherein R ¹ , R ² and R ³ are each hydrogen and Y is —CH ₂ —. The method of claim 1, wherein the octahydro-9-mercaptomethyl-6,10-dioxo-pyridazo [1,2-a] [1,2] diazepine-1-carboxylic acid is prepared. The method of claim 1, wherein the octahydro-9-mercaptomethyl-10-oxo-6H-pyridazo [1,2-a] [1,2] diazepine-1-carboxylic acid is prepared. The method of claim 1, wherein the decahydro-10-mercaptomethyl-6,11-dioxo-6H-pyridazo [1,2-a] [1,2] diazosine-1-carboxylic acid is prepared. 10. The method of any one of claims 1-9, wherein the coordination at the asymmetric carbon atom associated with the R ¹ -S-CH ₂ and R ² -OOC substituents is (S). ※ Note: The disclosure is based on the initial application.