公开(公告)号：US09902699B2

公开(公告)日：2018-02-27

申请号：US14437655

申请日：2012-10-24

Applicant: Gregory Rosocha

Inventor： Gregory Rosocha ,  Robert Batey

IPC: C07D217/02 ,  C07D217/04

CPC classification number: C07D217/02 ,  C07D217/04

Abstract: A procedure for the synthesis of tetrahydroisoquinolines from 2-methyl-1-phenyl substituted indene is described. The process involves the use of osmium tetroxide to cleave the indene double bond forming the keto aldehyde product, which is then combined with a substituted amine forming the substituted isoquinoline. Isoquinolines can be useful as industrial products in the chemical, agrochemical, oil and gas industry, as well as useful as medicaments in the pharmaceutical industry.

公开(公告)号：US20150274617A1

公开(公告)日：2015-10-01

申请号：US14437628

申请日：2012-10-24

Applicant: Gregory ROSOCHA

Inventor： Gregory Rosocha ,  Robert Batey

IPC: C07C23/18

Abstract: The present invention is a process to make 1-aryl-2-bromo substituted indenes and 1-phenyl-2-bromo substituted indenes that can have different functional groups present around the indene ring and/or the aromatic and/or phenyl ring. The indenes are made using the corresponding 1,2-biaryl-gem-dibromocyclopropane and/or 1,2-biphenyl-gem-dibromocyclopropanes and/or 1-aryl-2-phenyl-gem-dibromocyclopropanes using a metal salts, a solvent, low temperatures.

Abstract translation: 本发明是制备1-萘基-2-溴取代的茚和1-苯基-2-溴取代的茚的方法，其可以在茚环和/或芳族和/或苯环周围存在不同的官能团。 使用相应的1,2-二芳基 - 偕 - 二溴环丙烷和/或1,2-联苯基 - 二溴环丙烷和/或1-芳基-2-苯基 - -二溴环丙烷，使用金属盐，溶剂， 低温。

公开(公告)号：US10017479B2

公开(公告)日：2018-07-10

申请号：US14890731

申请日：2013-08-02

Applicant: Gregory Rosocha

Inventor： Gregory Rosocha ,  Robert Batey

IPC: C07D257/04 ,  A61K31/41 ,  B01J19/24

CPC classification number: C07D257/04 ,  A61K31/41 ,  B01J19/24 ,  B01J2219/00164 ,  B01J2219/00166 ,  B01J2219/2401

Abstract: A chemical process that can form pharmaceutically acceptable medicaments NNRTI's for the treatment of HIV starting from thiotriazole compounds. The chemical process can form thiotetrazoles such as 2-((1-(naphthalen-1-yl)-1H-tetrazol-5-yl)thio)-N-(2-nitrophenyl)actetamide that is. a potent NNRTI with nanomolar activity.

公开(公告)号：US10526262B2

公开(公告)日：2020-01-07

申请号：US14437628

申请日：2012-10-24

Applicant: Gregory Rosocha

Inventor： Gregory Rosocha ,  Robert Batey

IPC: C07C17/23 ,  C07C23/18 ,  C07C25/22 ,  C07C201/12 ,  C07C253/30 ,  C07C2/86 ,  C07D217/04 ,  C07D471/06

Abstract: According to embodiments described in the specification, a chemical process includes the steps of reacting a chemical reaction fluid including a solvent, 1,2-biaryl gem-dibromocyclopropane or 1,2-biphenyl-gem-dibromocyclopropane, and a metal salt including a silver tetrafluoroborate salt at low temperatures to make 1-phenyl-2-bromo indenes in a vessel that is capable of being closed.

公开(公告)号：US09932283B2

公开(公告)日：2018-04-03

申请号：US14437646

申请日：2012-10-24

Applicant: Gregory Rosocha

Inventor： Gregory Rosocha ,  Robert Batey

IPC: C07C29/32 ,  C07C1/00 ,  B01J19/00 ,  C07D217/04 ,  C07D303/48 ,  C07D471/06 ,  C07C2/86 ,  C07C201/12 ,  C07C253/30 ,  C07C17/23 ,  C07C23/18 ,  C07C25/22

CPC classification number: C07C29/32 ,  B01J19/0093 ,  B01J2219/00873 ,  B01J2219/0095 ,  B01J2219/00984 ,  C07C1/00 ,  C07C2/861 ,  C07C17/23 ,  C07C23/18 ,  C07C25/22 ,  C07C201/12 ,  C07C253/30 ,  C07C2602/08 ,  C07D217/04 ,  C07D303/48 ,  C07D471/06 ,  C07C205/12 ,  C07C205/55 ,  C07C255/57 ,  C07C205/37 ,  C07C13/465

Abstract: The cross-coupling reaction of 2-bromo-1-phenyl indenes with phenyl acetylenes or propargyl alcohol is disclosed. The cross-coupling reaction uses a palladium catalyst with triphenylphosphine in the absence of a copper co-catalyst. The reaction is carried out with pyrrolidine as the base in water at 120° C.