Patent classifications
C07C29/147
Processes for preparing alpha-necrodyl compounds and processes for preparing gamma-necrodyl compounds
The present invention provides processes for preparing an α-necrodyl compound of the following general formula (3): wherein R.sup.2 represents a monovalent hydrocarbon group having 1 to 9 carbon atoms, the process comprising: subjecting a 3, 5, 5-trimethyl-3-cyclopentene compound of the following general formula (1): wherein R.sup.2 is as defined above, and X represents a leaving group, to a nucleophilic substitution reaction with a methylating agent of the following general formula (2): wherein M represents Li, MgZ.sup.1, ZnZ.sup.1, Cu, CuZ.sup.1, or CuLiZ.sup.1, and Z.sup.1 represents a halogen atom or a methyl group, to form the α-necrodyl compound (3). The present invention further provides processes for preparing γ-necrodyl compounds of the following general formula (4): wherein R.sup.2 represents a monovalent hydrocarbon group having 1 to 9 carbon atoms, the process comprising: subjecting the α-necrodyl compound (3) thus obtained to a positional isomerization reaction at the double bond to form the γ-necrodyl compound (4). ##STR00001##
METHOD AND COMPOUND USEFUL IN PREPARATION OF OREXIN-2 RECEPTOR ANTAGONIST, AND LEMBOREXANT HAVING FEW IMPURITIES
The present application discloses a method and a compound that are useful for preparation of a compound of Formula (XI). Furthermore, the present application discloses the compound of Formula (XI) comprising a small amount of impurities.
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METHOD AND COMPOUND USEFUL IN PREPARATION OF OREXIN-2 RECEPTOR ANTAGONIST, AND LEMBOREXANT HAVING FEW IMPURITIES
The present application discloses a method and a compound that are useful for preparation of a compound of Formula (XI). Furthermore, the present application discloses the compound of Formula (XI) comprising a small amount of impurities.
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Fused cyclooctyne compounds and their use in metal-free click reactions
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Fused cyclooctyne compounds and their use in metal-free click reactions
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Fused cyclooctyne compounds and their use in metal-free click reactions
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Diester compound having a dimethylcyclobutane ring, a process for preparing the same, and a process for preparing dimethylcyclobutane compound derived from the diester compound
The present invention provides a process for preparing a diester compound of the following general formula (1), having a dimethylcyclobutane ring, wherein R.sup.1 and R.sup.2 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, the process comprising reacting a dimethylcyclobutanone compound of the following general formula (2), wherein R.sup.1 is as defined above, with a phosphonic ester compound of the following general formula (3), wherein R.sup.2 and R.sup.3 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, to produce the diester compound (1), having a dimethylcyclobutane ring. ##STR00001##
Diester compound having a dimethylcyclobutane ring, a process for preparing the same, and a process for preparing dimethylcyclobutane compound derived from the diester compound
The present invention provides a process for preparing a diester compound of the following general formula (1), having a dimethylcyclobutane ring, wherein R.sup.1 and R.sup.2 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, the process comprising reacting a dimethylcyclobutanone compound of the following general formula (2), wherein R.sup.1 is as defined above, with a phosphonic ester compound of the following general formula (3), wherein R.sup.2 and R.sup.3 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, to produce the diester compound (1), having a dimethylcyclobutane ring. ##STR00001##
Diester compound having a dimethylcyclobutane ring, a process for preparing the same, and a process for preparing dimethylcyclobutane compound derived from the diester compound
The present invention provides a process for preparing a diester compound of the following general formula (1), having a dimethylcyclobutane ring, wherein R.sup.1 and R.sup.2 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, the process comprising reacting a dimethylcyclobutanone compound of the following general formula (2), wherein R.sup.1 is as defined above, with a phosphonic ester compound of the following general formula (3), wherein R.sup.2 and R.sup.3 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, to produce the diester compound (1), having a dimethylcyclobutane ring. ##STR00001##
Methods of controlling hydroformylation processes
The present invention relates to methods of controlling hydroformylation processes for producing normal (N) and iso (I) aldehydes at a N:I ratio. In one aspect, a method of controlling a hydroformylation process comprises contacting an olefin with carbon monoxide, hydrogen and a catalyst, the catalyst comprising (A) a transition metal, (B) a monophosphine, and (C) a tetraphosphine having the structure described herein, the contacting conducted in one or more reaction zones and at hydroformylation conditions to produce a blend of normal (N) and iso (I) aldehydes at a N:I ratio, the method comprising at least one of increasing the N:I ratio by adding additional tetraphosphine to a reaction zone; decreasing the N:I ratio by adding additional monophosphine to a reaction zone; or increasing the N:I ratio by volatilization of the free monophosphine.