Invention Grant
- Patent Title: Electrophilic reagents for monohalomethylation, their preparation and their uses
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Application No.: US15001505Application Date: 2016-01-20
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Publication No.: US09359294B2Publication Date: 2016-06-07
- Inventor: Emilia Perpetua Tavares Leitao
- Applicant: Hovione Inter limited
- Applicant Address: CH Lucerne
- Assignee: Hovione Inter Limited
- Current Assignee: Hovione Inter Limited
- Current Assignee Address: CH Lucerne
- Agency: MacMillan, Sobanski & Todd, LLC
- Priority: PT105356 20101027; PT105942 20111018
- Main IPC: C07C317/00
- IPC: C07C317/00 ; C07C381/12 ; C07J31/00 ; C07J3/00

Abstract:
The invention provides a compound of formula A, B, C or D, methods for making them, intermediates therefor, and their use in making organic biologically active compounds: Wherein: X=F, Cl, Br, I, sulfonate esters, phosphate esters or another leaving group R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 are each individually selected from H, alkyl, aryl, alkynyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, nitro, halogen or amino; or are selected from H, C1-C10 alkyl, aryl, C1-C10 alkynyl, C1-C10 alkenyl, C1-C10cycloalkyl, C1-C10 cycloalkenyl, C1-C10 alkoxy, nitro, halogen or amino R11=tetrafluoroborate, triflate, halogen, perclorate, sulfates, phosphates or carbonates Excluding the case when: X=F and R1=R2=R3=R4=R5=H and R6=R7=R8=R9=methyl, R10=H and R11=triflate or tetrafluoroborate; or Wherein: X=F, Cl, Br, I, sulfonate esters, phosphate esters or other another leaving group; and R1, R2, R3, R4, R5 are each individually selected from H, alkyl, aryl, alkynyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxy, nitro, halogen or amino; or are selected from H, C1-C10 alkyl, aryl, C1-C10 alkynyl, C1-C10 alkenyl, C1-C10 cycloalkyl, C1-C10 cycloalkenyl, C1-C10 alkoxy, nitro, halogen or amino and R11=tetrafluoroborate, triflate, halogen, perclorate, sulfates, phosphates or carbonates; and R12=resin, naphthalene or substituted naphthalene Excluding the case when: X=F and R1=R2=R3=R4=R5=H and R6=R7=R8=R9=methyl, R10=H and R11=triflate or tetrafluoroborate and when X=F and R1=R2=R3=R4=R5=H and R12=poly(styrene-co-divinylbenzene) and R11=triflate or tetrafluoroborate; or Wherein: X=F, Cl, Br, I, sulfonate esters, phosphate esters or another leaving group R13=naphthalene or substituted naphthalene R6, R7, R8, R9, RIO are each individually selected from H, alkyl, aryl, alkynyl, alkenyl, cycloalkyl, cycloalkenyl, alcoxy, nitro, halogen or amino; or are selected from H, C1-C10 alkyl, aryl, C1-C10 alkynyl, C1-C10 alkenyl, C1-C10 cycloalkyl, C1-C10 cycloalkenyl, C1-C10 alkoxy, nitro, halogen or amino R11=tetrafluoroborate, triflate, halogen, perclorate, sulfates, phosphates or carbonates; or X=F, Cl, Br, I, sulfonate esters, phosphate esters or another leaving group R13=naphthalene or substituted naphthalene R11=tetrafluoroborate, triflate, halogen, perclorate, sulfates, phosphates or carbonates R12=resin, naphthalene or substituted naphthalene.
Public/Granted literature
- US20160130223A1 Electrophilic Reagents for Monohalomethylation, Their Preparation and Their Uses Public/Granted day:2016-05-12
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