TW211568B - - Google Patents

Description

A6 B6 V. Description of the invention (/) The present invention relates to a therapeutically active quinazoline compound > a method for preparing this compound > a pharmaceutical composition containing this compound * and a method for treating it 0 This novel compound is available Used in the preparation of psychological drugs > such as the treatment of neurological diseases »such as anti-m drugs» reduce anxiety, hypnosis »anti-psychotic> anti-vomiting» and used to improve the cognitive function of the mammalian brain > Or as an antagonist of diqizam. The antagonist 〇There is a combination of 1 1 4 — and 1 »5 — diazonaphthalene in the holding position of the central grip nerve of the spine. It is known (S q U i Γ e S > R • F • and B Γ ae S tr UP 9 C • 1 η N at U Γ e (L 〇η d 〇η) 2 6 6 (1 9 7 7) 7 3 (Please read the back side first; ± Issues before writing this page) Printed by the Employees Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 2-7 3 4) These positions are known as dikrypton naphthalene. It has now been found that many novel oxazoline and porazoline compounds have strong affinity for diazonaphthalene, so it can be used for the preparation of psychotropic drugs. Therefore, an object of the present invention is to provide this novel quinazoline compound.

The compounds of the present invention have the general formula I

Q \ fy The hydrated or retained acid-acceptable overwhelming medicine and the original paper ruler in Q and the applicable Chinese Western Standard (CNS) A 4 specifications (210 X 297 public goods) V. Description of the invention (Λ) A6 B6 (Before you read the back: Jade Matters and then write this page) Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs

0-N

0 — N

N a 0

R -C where either C, c straight chain is gas-based 0 0 R 1 or branch 7 — is c, c acyclic amine ring or daughter, oxygen, sulfur, a non-R s or -c N; is hydrogen , C3 _7 6 straight-chain or branched CS alkyl substituted C _7 6 oxy-Cl—S — C is -alkyl; and R z are hydrogen, C i cycloalkyl 1 _s Substituted cycloalkyl, Ci_s alkoxyalkyl or trifluoromethyl; R8 is

, Di-C alkane Cycloalkyl, Y-oxy-6 — Y-in-one, copper condensate, base, in .sulfinyl ring or ring

One or more of CC 1 _ R 4 I, trialkyl, 〇-hydroxy, R 5 fluoromethyl C 2 _ or R 2 and the ring in the ring, sulfide-like _, _ s alkylalkyl Or, R 6 points. Nitro, s alkenyl substituted C! _ C 1 _, methyl R 2 and the system, the acetyl group or these rings, C! Phenyl group is a hydrogen amine group, C 2 Base, aminoaminopyridinyl, alkylalkyl, CC! — Nitrogen atom formation or multi-value—hospital 6 m. 6-homoyl—one health carbonyl system _ 8 substitution, hydroxyl radon basic paper size is suitable for home Standard (CNS) A.1 regulations (210 X 297 male) Selectively substituted with C, phenyl, or R 2 and R 3

C alkanes 1 _ 6 —Yuan oxygen 6 Yuan or one of the 4-6 original carbon atoms can be exchanged with m, or each of its hydration can be selectively alkoxy-methyl, hydroxy group, C 1, B r, F, linear or branched C i _ alkyne® group, C 1 _ 6 A6

Fifth, the description of the invention (3) (: #First read-, back of the page; ± -item and then write this page) Hospital air base, Cl _ S home air base_Cl _ 6 home base or Ci _ S-home oxygen Carbonyl; the restriction is that when Q is

When R4, R5, R * 5, R7 can not be hydrogen at the same time; where R1 'is H, Ct _s alkyl or unsubstituted C3 _7 cycloalkyl; R2 and R3 are H, Ci _ 6-alkyl gas group , C 3 -7 cycloalkyl or Ci + s —alkyl or NR 2 R 3 forms an unsubstituted morpholine or thiomorpholine; and the compound of formula I is not ethyl 6 —atmosphere 5 —morpholine squint Azole [1, 5-a] quinazoline _ 3 -carboxylic acid ΘΙ or 6-atmosphere 3-(3-cyclopropyl 1, 2, 4:-well 5-yl)-5-morpholine An azole azole [1, 5-a] oxazoline. The present invention also relates to methods for preparing the above-mentioned compounds. These methods include the printing of a compound of formula II and formula III by employees ’cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs.丨 3 · (210 X 297 Gongbo) A6 B6 V. Description of the invention ()

7 R

Y (II) where R2, R3, R4, R5, only 6 and P7 are as defined above, where Y is a leaving group, CN-CHz-Q (III) where Q is as above Definer, to form a compound of formula I, or b) reacting a reactive derivative having the general formula IV compound and a compound having the general formula V ··

COOH (keep reading the notes on the back of the board before writing this page) (IV) where R2, R3, R4, R5, R6 and R7 are as defined above, printed by the Staff Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs system

Rl-C (= NOH) NHz (V) where R1 is as defined above to form a compound of formula I, where Q is the S3 home standard (C! VS) A4 standard ( 210 X 297 gong) V. Description of the invention (Γ) 0-Ν

R where R1 is as defined above, or c) reacting a compound of formula VI with a dehydrating agent,

Α6 Β6 (VI) wherein R2, R3, R4, R5, R6 and R7 are as defined above to form a compound of formula I, wherein R2, R3, R4, R5, Rs and R7 are as defined above And where Q is a radon group, or d) reacts a compound of formula VI I with NH2〇H,

(VII) ------------------------- ^ ------ '玎 ------ ^ (Please read the back of 汸 first (Notes to be written on this page) Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs where R2, R3, R4, R5, Rs and R7 are as defined above to form a Formula VI II compound. SK Family Standard (CNS) Grade A (2 丨 Ο X 297 Gongshi)

A6 __B6_ 5. Description of the invention (4)

OH (VIII) where R2, R3, R4, R5, RS * R7 are as defined above, and the compound of formula VI II and R1 — COOEt or (R1 CO) 2 0, where R1 is as As defined above, to form the compound of formula I, where Q is (please read the precautions on the back before writing this page) 丨 Installed-N-0

R1 where R1 is as defined above, or e) hydrolyze the compound of formula I to form the compound of formula IX line 7

Printed by the Employee Consumer Cooperative of the Central Bureau of Standards of the Ministry of Economy where Q, R 4, R ^. ^^^ and ruler 7 are as defined above, and the compound of formula IX and P0C 13 are formed to form the compound of formula X-10- This paper The standard is applicable to the Chinese National Standard (CN'S) A 4 cash (2ί 0 X 297 g: ^) Printed by the Consumer Consumption Cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs

It reacts with a compound of formula XI NHR 2 R 3 (XI) where R2 and R3 have the above definitions to form a compound of formula I leaving group Y can be any patent No. 4, 0 3 1. For example, halogen, alkyl sulfide Nitrosoalkylamine group, R) z, where R is less than 2) 2, where R ′ reacts with the nitrogen atom, azyl group, or methylmethine under the conditions of its contact, or sodium ) The alkoxide in the base is carried out in an organic solvent. There is no under the reaction chopsticks. It is an anhydrous aprotic solvent.

He's combined 0 7 9 group, such as alkyl chloro group, hydrogen sulfonyl group, an OP (lower alkyl group or a 0 P For example, described in the United States No. 9, 4 2 0 in the appropriate group group, or 4.3 5 such as methylthio, aralkylthio, N-R "represents lower together represents a heteroethyl group to two as one or hydrogenation. This is reactive. Like in diazahexyl β base , The material is the preferred organic solvent, except for methylformaldehyde 11-

(Ο) (grade alkyl or, like morpholine, this reaction is more in alkali metals. This reaction is anti-plaque and a water-insoluble (DMF Ο) (Ο NRJR phenyl, or phenyl, pyrrole is in (eg, potassium The better one is the reaction production part i, which is better). The paper size of the tetrahydro-stranded book is the Chinese In-House 1? Standard (CNS) A 4 regulation _ grid (210 X 297 public goods) 上 丄 '·' i ο A6 B6 Printed by the Employees ’Cooperative of the Central Bureau of Standards of the Ministry of Economy V. Description of invention (δ) Furan (T Η F)» or its analogue 〇 The temperature used can be any suitable for this reaction-proceed at an appropriate speed And the temperature that does not decompose > is usually from a 40 to about room temperature m. It will be suitable for other applications. The starting materials used in the synthesis of compounds of formula I are known or can be prepared from commercial materials in a conventional manner. Get> As per Ka Γ mi η S kieta 1 • »J • E η V i Γ 〇η • SG i • Η ea 1 tht P a Γ t B i 1 9 8 3 Β 1 8 (4 — 5) 5 9 9 〇 copies The pharmacological properties of the compound can be determined by the ability of the diazonaphthalene to replace the f 1 U η it Γ a Z e P am indicated by the radioactivity m. The ability of the compounds of the invention to be substituted can be determined by determining the value of ED 5 〇 It is determined that the ED 5 〇 value represents the dose of the test substance which causes a specific combination of 3 Η — f 1 U η it Γ a Z e P am and diazonaphthalene (mg / kg) in the living brain to a reduced value 50% 〇 This in vivo test was implemented according to the method described in US Patent No. 4 * 7 7 4 I 2 4 5. The results of the test of the compound of the present invention are listed in the following Table I. Table I Compound ED 5 〇1 2 9 ο 〇 • 4 4 2 0 〇 • 2 9 2 4 0 5 -12 (please read the precautions on the back of 汸 before filling out this page). Install. Line. This paper size is applicable to China National Leng Zhun (CNS> A4 clam (210 X 297 mm) A6 B6 printed by the Ministry of Economic Affairs Central Standards Bureau staff consumer #cooperative society V. Description of the invention (,) The compound of the present invention and a traditional adjuvant, carrier , Or diluent, and if necessary, in the form of its pharmaceutically acceptable acid additions, can be administered in the form of its pharmaceutical composition and unit amount, and in the form of solid sulfide, such as tablets or fillings Capsules, or liquid forms, like solutions, suspensions, emulsions, adjuvants, or capsules filled with these substances, all taken orally, or in the form of plugs suitable for rectal treatment; or parenteral (including subcutaneous The form of sterile injectable solution. The formation of this pharmaceutical ingredient and its unit dose may include traditional ingredients in traditional proportions, with or without additional active compounds or ingredients, and this unit dosage form may contain any suitable effective amount of activity to reduce boredom in the middle-grip nerve system Ingredients, which are the daily intended dosage range. Tablets can be, every tablet, containing 0.1-100 mg of active ingredient, with a range of 1.0-50 mg is a representative of a suitable unit dosage form of the present invention. The compounds of the present invention can be used in the formulation of pharmaceutical preparations, for example, for oral and parenteral administration to mammals entrapped in humans, in accordance with traditional Ga 1 e η's medical methods. Traditional excipients are organic or inorganic carrier substances that are acceptable for hair release and are suitable for non-suiwan or oral use without adverse reactions with the active compound. Examples of such carriers are water, aqueous solution of saline, ethanol, polyethylene glycol, polyhydroxyethoxylated sesame oil, gelatin, lactic acid, amylose starch, magnesium stearate, talc, silicic acid, fatty acid monoglyceride and Fatty acid diglyceride, pentaerythritol fatty acid ester, hydroxymethyl cellulose and polyvinylpyrrolidone. Disinfect and mix the pharmaceutical preparations with supplementary ribs if necessary, supplementary ribs-13- ------------------------ installed ------- -玎 ------ Line f is familiar with the notes on the back and then write this page) This paper scale is applicable to the Chinese and Western standards (CNS > A Ο 見 格 (210 X 297 公 *> 81.9 .20,000 · Printed A6 B6 by the Employee Consumer Cooperative of the Ministry of Manchurian Economy. V. Description of invention (Ισ), such as lubricants, stabilizers, wetting agents, emulsified rain, shadow osmotic pressure, buffer And / or coloring substances, etc., will not be destroyed by sleeping with the active compound. Non-enteric use, especially suitable for injectable solutions or suspensions, preferably active compound dissolved in polyhydroxylated sesame oil Form an aqueous solution. Ampoules are convenient unit dosage forms. For oral use, tablets, sugar-coated tablets or capsules with talc and / or hydrotalcite-containing compounds or conjugates, etc. It is preferably lactose and / or Yi-type source powder and / or yam potato starch. When sweetening excipients are used, slush, syrup or the like can be used. A wider range of the compounds of the present invention are formulated in unit placement form, containing 0.05 to 100 mg in a unit dose pharmaceutically acceptable to contain fish. Typical tablets can be completed by traditional tablet manufacturing techniques, which include: active compound 1. 〇mg lactose 67.3mg ph.Eur

Avicel 31.4 mg

Aiberlite IR P 38 1.0 mg stearic acid il 0.25 mg ph.Eur Because the compound of the present invention has a high affinity for dikryptonnaphthalene. It is quite effective in the treatment of neurological disorders or insufficiency in the middle. It is effective. The amount can be reduced, to change the bodhisattva or eliminate the disease. The important central nervous system activities of the compounds of the present invention include antispasmodic, anxiolytic, hypnotic, antipsychotic, and antivomiting activities, which are modified with low toxicity to mammals. Standard (CNS) A 4 specifications (210 X 297 g; Ϊ > ------------------------ installed —.——. 玎 --- --- Line. (Please read the precautions on the back of it before filling in this page) 丄 丄 d A6 B6 V. Description of the invention (丨 丨) (Qi first read: »'Notes on the back of the page and then write this page) The function of brain cognition, and its existence has the most effective medical guidance. The compound of the present invention can be administered according to this, the object is a living animal or human body, used to treat, alleviate, improve or eliminate the symptoms and the neurological system Diazonaphthalene is certified and needs this psycho-medical treatment, for example, to treat spasticity, insomnia, anxiety, psychosis, vomiting, suspense, and / or as a kryptonine receptor antagonist, In the form of pharmaceutically acceptable acid addition salts (such as hydrogen bromide, hydrogenated hydrogen, tartrate, or sulfate sulfate), if necessary, prepared from common or traditional methods In any event, such as evaporating the free base and acid together in the solution), usually together. It coexists with a pharmaceutically acceptable carrier or diluent, and is preferably present in the form of a pharmaceutical composition. Rectal or parenteral (including subcutaneous) methods to reduce the effective dose of psychopharmacological central nervous system diseases, such as primary antispasmodic, anxiety, hypnotic and / or antipsychotic doses, effectively reduce central nervous system The effective cut of traditional diseases is due to the affinity for the diazonaphthalene receptor. The appropriate dose is 1 'to 200 mg per day, 1 to 100 mg per day, and 1 to 30 mg per day, as usual According to the correct medication method, medication form, medication for symptomatic treatment target, target weight, and the preference and experience of the doctor or veterinarian% The sex example printed by the employee consumer cooperative of the Central Bureau of Standards of the Ministry of Economic Affairs 3 The cost limit is not the same as described in the first step. 3 Pyridin-5 4 azole, squint 2 _, yl 1 methyl-fluorotripropyl-cyclo 6} linyl azole | quine 5] I a ίpent I nitrogen 5 two , Oxygen 1 paper ruler and applicable tHK home standard (CNS) A4 cash (2L0 X 297 g; ^) ~ ^ E ^ 2ll0t3 Λ6 B6 V. Description of invention (1) Compound 1) Central Bureau of Standards, Ministry of Economic Affairs Printed by Gugong Cooperative Cooperative in 2 * -chloromethylene 4-monomorpholine-5 monotrifluoromethyl-oxazoline (6 〇0 m 8 > 1 9 mm 〇1) and 3-cyclopropyl — 5 — Isocyanomethyl — 1 > 2 »4 — Oxydiazepine S (4 4 0 mgt 2 • 9 mm 〇1) dissolved in a solution of anhydrous D MF (1 5 m 1) > in Under a nitrogen atmosphere and 5-10 TC. Add solid ammonium-butyrate (3 3 〇mg »2-9 mm 〇1) t within the temperature range and mix at a temperature of 5-10 V This mixture was 〇 • 5 hours> and ground with water (2 〇m 1) 〇 filtered out crystal 1 and washed with water (1 〇m 1) and ethyl acetate was poured into the final purification is to mix this crystal m (1 〇m 1) in acetone> 3 3 〇m 8 of the title compound »m • P • 1 9 ~ 7 — 1 9 9 v 〇1 Η η mr 3 (CDC 1 3): δ 8 • 4 (S »1 Η t 眯 azole—) 9 8 • 2 — 7 9 (m» 3 Η »benzo—) 4 • 〇— 3 • 2 (mt 8 Η »morpholinyl one) * 2 • 2 (mr 1 Η» C Η), 1 bis 3 — 1 * 0 (m > 4 Η t C Η Z) 〇Example 2 — (3 — Cyclopropyl — 1 »〇» 4 — oxydiazepine 5 — yl \ — 6 — methyl — 5 — m porphyrin — benzozole r 1 > 5 — a] Quinazoline (Compound 2) A mixture> including 2 — ammonia — 5 — methyl — 4 — morpholinyl — oxazoline (1 • 6 8 g * 6 • 4 mm 〇1) and 3 — cyclopropyl- 5 — iso-m-methyl Base — 1 »2 * 4 — Gas dinitrogen (1 9 8) Dissolve -16-, (-read first ';: 1'. The back of it; ±-? Item and then write this page) Binding 'Order.-Line This paper ruler Λ is applicable to China S Jiafuzhun (CNS) Grade 4 (210 X 297 public goods) 211〇βύ Printed by the Employees Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs Ming (丨 s) in 15 m 1 of anhydrous dimethylformamide > Cool it to 0 V > and slowly add tert-butyrate gas (1 • 4 g > 5 minutes) ; 1 2 5 mm 〇1) »The temperature is kept at 1 0 〇 Mix the mixture at room temperature for two hours i and then to 0 ° C 〇 Collect the crystallized Zrh OL precipitate f in the dropper with ethyl acetate Esters and washed with water iSW m »After drying, the title compound is obtained as pale yellow crystals» m P. • 1 6 2 — 2 6 6 > yield 1 • 2 9 g 〇1 Η η m Γ δ (CDC 1 3 ) δ: 8 • 3 〇 (S > 1 Η > 眯 azole—) 7 • 8 5 — 7 • 3 5 (m 3 Η »benzo-I) > 4 〇5 — 3 8 (m > 4 Η »Ν — C Η 2)» 3 • 7 5 — 3. 3 〇 (mt 4 H * 0 — C Η 2) > 2 3 8 (S »3 Η» C Η 3) y 2 * 3 0 — 2 • 1 2 (m »1 Η t C Η) y 1 3 — 1 • 0 (m > 4 Η > C Η ζ) 〇 Prepared in a similar way Column compound 6 — bromo — 3 — (3 — cyclopropyl — 1, 2 > 4 — oxodimethane-5 — yl) — 5 monomorpholine — quinazoline C 1) 5 — a) quinazoline ( Compound 3) V m • P • 2 7 5 — 2 7 7 ° C »From 2 — Chlorine — 5 — Bromine — 4 — Morinyl — Quinazoline and O—Cyclopropyl — 5 — Isoradyl methyl — 1 > 2 »4 — prepared by gas diazoxide; tert-Butyl 6 monomethyl— 5 — thiomorpholinyl — zonazo C 1» 5 — a Ί J oxazoline — 3 — carboxyl Ester (Compound 4) m Ρ • 1 6 4 — 1 6 6 »Reaction from 2 — atmosphere — 5 monobromo — 4 — thiomorpholinyl — quinazoline and tert-butyl isocyanoacetate Prepared; -17- (-" read-, back:; i-fJfi and then write this page) This paper scale is suitable for China K Jiazheng (CiVS) A 4 specifications (210 X 297 mm) A6 B6 2li〇6d Fifth, the description of the invention (丨 red) 6-bromo-3-one (3-cyclopropyl-yl)-5 (N — (2) amino group) — benzozole Γ 1 1 5-P • 1 7 〇— 1 7 1 X: > — (2 t 2 — dimethoxyethyl 3 — cyclopropyl one 5 — Isocyanomethyl. Prepared 1 3 — (5 — Cyclopropyl — 1 »2 6 — Methyl — 5 — Thiomorpholine — Compound 6) m • P • 2 〇— Methyl — 4 — Thiomorpholinyl —% ylmethyl — 1 »2 * 4 — Oxygen 6 — Mo — 3 — (3 — Cyclopropyl — yl) — 5 — (N — Ethoxyphenazole C 1> 5 — a Quinazoline 9 — 1 9 1 t: 9 consists of 2 — nitrogen — ylmethyl — N — methylamino) — cyanomethyl — 1 ♦ 2 > 4 — oxygen 7 — atmosphere — 3 one (3 Cyclopropyl-yl) — 5 — (N »N — bis-acidazole r 1 1» 5 — a] Quinazol 1 2 — 2 1 5 V »from 2 t 6 — methoxyethyl) amine group) One m ------------------------ installed ------, 玎 ------ ^ (mu first read the back of 汸; ± Please fill in the form and page again) Printed and burned by the Ministry of Economic Affairs Central Standard Residence Staff Consumer Cooperative -1, 2, 4-oxydiazepine S-5 2-dimethylaminoethyl) N-methyl a] quinazoline (compound 5), m

Made from 2-—5_bromo-4— (N) —N-methylamino) oxazoline and 1,2,4-oxydiazepine S, 4-gas diazepine_3_yl) _ 眯 azole [1, 5-a] oxazoline (5-206Ό, prepared from 2-gas-5quinazoline and 5-cyclopropyl-3-isodiazepine S; 1, 2, 4 — Gas dioxo-5 carbonylmethyl-N-methylamino) (compound 7), m. Ρ · 18 5-bromo-4- (N-ethoxycarbonylquinazoline and 3-cyclopropyl A 5-isodiazepine is prepared by cracking; a 1, 2, 4- gas diazino-5 (2-methoxyethyl) monoamine) Lin (compound 8), mp 2 one two gas one 4 (N, N — bis (2 oxazoline and 3-cyclopropyl-5 — isoradon 18- This paper scale is common to the Chinese Western Standard (CNS> A 4 specifications (210 X 297 gongs »81.9.20,000 Ministry of Central Standards Administration. «Industry and consumer cooperation Thorium seal 5 < f · A6, B6 V. Description of invention (Ir) The preparation of methyl 1, 2, 4- gas diazoxide; 7 — atmosphere 3 — (3 -Cyclopropyl 1, 2, 4-gas diazenium-5-yl)-5-(N-(1, 3-dioxane-2-yl)-methyl-N- Methylamino) quinazoline [1, 5-sl] quinazoline (compound 9), mp 223-226C, consisting of 2, 6-diamine 4-(N-(1, 3-dioxane mono 2-yl) methyl-N-methylamino) -quinazoline and 3-cyclopropyl-5-iso-radonylmethyl-1, 2, 4 are prepared by gaseous diazepine; 3-(3 —Cyclopropyl-1, 2,4 monofluorodiazepine S — 5 —yl) — 7 —gas-5 morpholine quinazoline C1, 5 — a] oxazoline (compound 1〇), mp 243-2451 , Prepared from 2-gas-6-fluoro-4_morpholinyl-quinazoline and 3-cyclopropyl-5-isomylmethyl-1, 2, 4-oxodiazepine; ethyl 7-Fluoro-5-morpholinyl-quinazole [1,5-a] quinazoline-3-carboxylate (compound 11), mp 238-239t, composed of 2-ambient-6-fluoro-4- It is prepared from quinolinyl-quinazoline and ethyl isocyanate; isopropyl 7-chloro-5- (N- (1,3-dioxan-2-yl) methyl-N-methylamino) squint Azole [1, 5-a] quinazoline 3-carboxylate (compound 12), m.p. 1 3 5-1 3 7 TC, consisting of 2, 6- two gas one 4 one (N-(1 , 3 — Erninyuan_2_ group) -methyl-N-methylamino) quinazol tablets and isopropyl isocyanoacetate prepared; -1 9- This paper is suitable for the West China standard (CNS) V 〇See grid (210 X 297 public goods) 81.9.20.000 ------------------------ installed ------. TΓ ------. ^. (Please read the notes on the back of Qi first, and then write this page) 0 0 Central Bureau of Standards, Ministry of Economic Affairs R Gongxiao Φ Cooperation Thorium Seal 5th Generation Α6 Β6 V. Description of Invention (ις) 9 One atmosphere 3 — (3-cyclopropyl 1, 2, 4 — gas diazenium -5- monoyl) — 5-morpholine quinazoline [1, 5-a] oxazoline (compound 13), m.p. 121-124C, cracked by 2, 8 — dioxin-4 4-garolinyl_quinazoline and 3_cyclopropyl-5-isocyanomethyl-1, 2, 4_oxodi MS Prepared; 9-Gas 3-(3-Cyclopropyl-1, 2, 4-Gas diazepine-5 monoyl)-5-(4-Methyl-1 1 pair of diazahexyl) [1, 5-a] quinoline (compound 14), m.p. 1 9 9-20 It :, consisting of 2, 8-diamine mono 4-(4-methyl-1 1 one-to-two Azahexyl) -quinazoline and 3-cyclopropyl-5-isohydrogenmethyl-1,2,4-gas diazide S Prepared; 6, 9- dichloromethane 3-(3-cyclopropyl 1, 2, 4-oxodioxi 5-5-yl)-5-morpholine-azoazole [1, 5-a] Quinazoline (compound 15), m.p. 1 8 4-1 8 6 ° C, from 2, 5, 8-three atmosphere _ 4-quinolinyl quinazoline and 3-cyclopropyl-5- Isohydromethyl-1, 2, 4-oxodiazepine S is prepared; 7-gas-3 (5-methylaminomethyl-1,2,4-gasdiazepine-3-yl) -5 -(N-ethyl-N-methylamino) quinazoline [1,5-a] quinililine (composite tree 16) P. 169-1 7 2 t :, from 2, 6-diamine-4 -(N-methyl-N-ethylamino) -quinazoline and 3-isocyanomethyl-5-methoxymethyl-1, 2, 4-oxodiazepine; 3 — (3-Cyclopropyl 1, 2, 4-gas diazenium-5-yl) 1-20- This paper scale is applicable to the Chinese and Western National Standards (CNS) Jia 4 said grid (210 X 297 public goods) 81.9. 20.000 ------------------------ Pretend ------, 玎 ------ ^ (Recognize the first reading-the note on the back (If you are busy, please fill out this page)

Printed by the Central Bureau of Standards of the Ministry of Economic Affairs 1 * printed by the China Consumers ’Cooperation Fund * '1. V. Description of the invention (I 1) 5 —thiomorpholine-6 —trifluoromethyl monobenzotriazole [1, 5 — a] oxazole Porphyrin (Compound 17), m. Ρ · 162 — 165t, consisting of 2 — 4 — thiomorpholinyl — 5 — trifluorinated methyl oxazoline and 3 — cyclopropyl — 5 — isoradon Methyl-1,2,4-oxodinitrogen S is prepared by cracking; 3- (5-cyclopropyl-1,2,4-gas diazenium-3-yl) -5-thiomorpholine-6 —Trifluorinated methyl quinazoline [1, 5 — a] oxazoline (Compound 18), τη. P. 155 — 158 =, by 2-a 4-thiomorpholinyl 5-three gas Prepared by methyl quinazoline and 5-cyclopropyl-3-isogasylmethyl-1, 2, 4-pyrazine; 6-amino-3- (5-cyclopropyl-1 , 2,4 oxydioxa-3-yl) -5-morpholine-quinazoline [1,5-a] quinazoline (Compound 19), m.ρ · 184-187 ^ 0, from 2-gas A 5-amino group-4 morpholinyl-quinazoline and 5-cyclopropyl-3-isoaminomethyl-1, 2, 4-oxodiazepine S prepared; 3 — (3 — ring Propyl-1 , 2, 4-gas two gas S-5-yl)-6-fluoro-5-morpholine quinazoline [1, 5-a] quinazoline (compound 20), m. P. 2 1 6-2 At 1 8 ° C, it is prepared from 2-fluoro-5-fluoro-4-morpholinyl-quinazoline and 3-cyclopropyl-5-iso- radonylmethyl-1, 2, 4-gas diazoxide Get; 3-(5-cyclopropyl-1, 2, 4, 4-gas diazo S-3-yl)-6-fluoro-5-morpholine-myrazole [1.5-a] quinazoline (compound -2 1- This paper ruler is suitable for AA standard (CNS) Grade 4 specifications (210 X 297 public goods) 81.9.20,000 --------------------- --- Installation ------, 玎 ------ Φ. (Please read first-the notes on the back and then fill in this page) Employee consumption cooperation of the Central Standards Bureau of the Ministry of Economic Affairs ;: Yiyin A6 B6 V. Description of the invention (丨 Ϋ) 2 1) > m • P • 2 〇4-2 〇7 X: from 2-gas-5-gas-4-morpholinyl-quinazoline and 5-cyclopropyl — 3 — Isoradyl methyl — 1 »2 > 4 — gas two mm prepared to get 3 one (3 — cyclopropyl — 1 > 2» 4 — oxydiazepine — 5 Radical) — 6 — fluoro- 5 mono (cis — 2 »6 — dimethylmorpholine) — zonazo r 1 t 5 — aj quinazoline (compound .2 '2) tm-P • 1 S 7-1 8 8 > from 2 — gas — 5 — heat — 4 — (cis 2 t 6 — dimethylchrysolinyl) — quinazoline and 3 — cyclopropyl — 5 — iso% ylmethyl — 1 »2 > 4 — gas di η cracked to prepare 3 — (3 — m propyl — 1 1 2 > 4 — oxydiazepines — 5 — yl) — 6 — m — 5 — thiomorpholine-triazole C 1 5 — a] Quinazoline (Compound 2 3) »m • P • 2 5 2 — 2 5 3» From 2 — atmosphere — 5 — fluorine — 4 — benzomorpholinyl — quinazoline and 3 — * Cyclopropyl — 5 — isoamidomethyl — 1, 2 »4 — oxydiazepine is prepared from 3 — (3 — cyclopropyl — 1 t 2 > 4 — gas diazono — 5 — group) — 6 monofluoro— 5 — (4 — methyl — 1 — p-diazepine) — zonazo C 1 * 5 — a] Quinazoline (compound 2 4) m • P 2 5 8 — 2 6 0 »from 2 — fluorine — 5 — gas — 4 — (4 — methyl — 1 — p-dim hexyl) — quinazoline and 3 — cyclopropyl — 5 — Iso% ylmethyl — 1 > 2 > 4 — prepared by gaseous diazide to give 3 — (5 — cyclopropyl — 1 > 2 »4 — oxydiazepine — 3 — yl) — 5 one (Reverse 2 »5 — dimethylmorpholine) — 6 — — zonazole C 1» 5 a 3 quinazoline (compound 2 5) > m P 2 0 8 — 2 1 -22- --- --------------------- install ------ tr ------ line (please read the note on the back of ¾ * items before filling this page ) This paper ruler is applicable to the Chinese S Family Standard (CNS) Grade A 4 (210 X 297 mm) 81.9.20,000 V. Description of the invention (丨 1) < Please read the back of the Qi; please fill in the matters before the reading (This page)

Ot. Consists of 2-ambient 5-fluoro-4 4- (2,5-dimethylmorpholinyl) -quinazoline and 5-cyclopropyl-3-isomylmethyl-1, 2, 4 in one gas It is prepared by diazoxide; compound 25 is obtained from compound 26 by column chromatography, (lavage agent: ethyl acetate: acetone (2: 1)); 3-(5-cyclopropyl 1,2,4-oxodiazepine-3-yl) -5- (cis-2,5-dimethylmorpholine) -6-fluoro-quinazoline [1,5-a] quinazoline (Compound 26 ), m. p. 186 — 18 9t, consisting of 2-fluoro-5-fluoro-4- (2, 5-dimethylmorpholinyl) -quinazoline and 5-cyclopropyl-3-isohydrogen Methyl-1,2,4-oxodinitrogen S is prepared by cracking; compound 26 is obtained by column chromatography of compound 25, (washing agent: ethyl acetate: propionate (2: 1) ); 3 — (3-cyclopropyl-1, 2, 4-gasdiazepine S — 5-yl)-8-fluoro-5-morpholinyl-quinazoline [1, 5-a] quinazoline ( Compound 2 7), m.p. 276-27810. From 2-chloro-7-gas-4-morpholinyl-oxazoline and 3-cyclopropyl-5-isoradylmethyl-1, 2, 4-Oxydiazepine S is prepared by splitting; Ministry of Economic Affairs Central's standard residence staff consumption cooperation thorium printing frame 3-(3-cyclopropyl 1, 2, 4-gas dikrypium 5-yl)-5-(3, 3-dimethyl chrysoline) 7-fluoro-quinazoline [1, 5-a] quinazoline (compound 28), m.p. 259C, consisting of 2-chloro-6-fluoro-4 4- (3, 3-dimethylmorpholinyl ) A quinazoline and 3_cyclopropyl- 5-iso- radonyl methyl 1, 2, 4--gas diazocrack -23- 81-9.20.000 sheet paper is suitable for Chinese and Western S? Quasi (CNS> A 4 present grid (210 X 297 g: S) 垤 济 邡 中 採 測 標 樂 局 1 * Industry and Consumer Cooperatives printed «iiotiO A6 _ ^ _ B6_ Fifth, the invention description Uo) available; 3 — (3_ Cyclopropyl-5-isoxazole) -6-fluoro-5-morpholinyl-quinazoline [1,5-a] quinazoline (compound 29), m. Ρ · 208-2 1 0C, by 2 -Atmosphere-5-fluoro-4-morpholinyl-quinazoline and 3-cyclopropyl-5-iso- radonylmethyl-isoxazole; 3-(5-cyclopropyl-1, 2 ·, 4-oxodiazepine S-3-yl) — 5-(3, 3-dimethylmorpholine) -7-fluoro-quinazoline [1, 5-a] quinazoline (compound 30), m . Ρ. 251 — 254¾ By 2-ambient-6-fluoro-4- (3. 3-dimethylmorpholinyl) -quinoline and 5_cyclopropyl_3-isopropylmethyl-1, 2, 4--dichloro Nitrogen is prepared by cracking; tert-butyl 6-gas-5-morpholine-triazole [1, 5-a] quinileline _3_ carboxylate (compound 31), m.P. 19 1-19 3 ° C, prepared from 2-oxo-5-fluoro-4-morpholino-quinazoline and tert-butyl iso- radonyl acetate; 3 — (5-cyclopropyl-1, 2 , 4-chlorodiazepine-3-yl) -7-gas-5— (4-methyl-1-1-p-diazinocycloyl) quinazoline [1, 5-a] quinazoline (compound 32) , m. p. 2 0 2-2 0 4 ^, consisting of 2-amino-6-fluoro-4- (4-methyl-1-p-diazohexyl) _quinazoline and 5-cyclopropyl A 3-isoradonyl methyl 1,2, 4-gas diazepine prepared; 3-(3-cyclopropyl 1, 2, 4-gas diazo S-5-base)-5 -(N-(1, 3 -dioxane-2-yl) methyl-N-methyl-24- This paper scale is commonly used in Chinese and Western a-frame standard (CNS> A4 present grid (210 X 297 mm ) 81.9.20,000 ------------------------ installed ------ ΤΓ ------ line (read the back first) (I |) Α6 B6 amino group) 6-fluoro-quinazoline [1, 5-a] quinazoline (compound 3 3), m. P . 2 0 9-2 1 It :, from 2-ammonia-4-(N methyl-N-methylamino)-5-isocyanomethyl-1, 2 3-(5-fluoro one mile .4 —Gas diazepine 3-(5 -ring 5-(dioxaline and 3 S prepared —2-yl) —cyclopropyl mono-a] ° C, from quinazoline 3, 3 quinazoline propane Derived from the base one-dimethyl; 1, 2., 4-ylmorpholino) (compound 3 4), 2-ambient and 5-cyclopropyl-4 — (3, 3 — a 3 _isoventrious oxydio Nitrocyl-3-yl) -6-fluorofluoromazole [1, 5 m P. 210-212 dimethylmorpholine) -5_fluoro-ylmethyl-1, 2, 4-oxodiazepine S-crack Prepared; 3-(5-(脞 [1 5 -cyclopropyl-1, 2, 4-m-diazo S-3 -yl)-cis-2, 6-dimethyl-1-cyclopropanyl) A 6-qi Yimei, 5-a] quinazoline (compound 3 5 6 4 t: m. P. 6 3-1 1 a nerzyl)-5, by 2-Qi Yi 4 a central government Printed by Standard General Staff Cooperative Society ¾ Fluoro-quinazoline It is prepared by one gas and two ms; 1,2,4 7 -fluoro- 5 -thiophosphorinoline-conazole [2, 4 -ylmethyl _ 1, 3-(5 _ cyclopropyl (cis-2, 6-di Methyl one and 5_ cyclopropyl one 3-iso- radon gas di SS_3_ group)-1, 5-a] quinazoline (chemical 235t, from 2-atmosphere one 6 5-cyclopropyl one 3-different gas Base compound 36), m.p. 2 3 3-monofluoro 4 _ thiomorpholine-oxazoline and methyl one 1, 2, 4-oxydiazepine prepared; 3-(3- Cyclopropyl-1, 2, 4-gas diazenium-5-yl) -25- This paper scale is applicable to the aa family standard (CNS) Grade A 4 (210 X 297 public goods) 81.9.20,000 ---- --------------- 1 ----- installed ------, 玎 ------ line (please read the commemorative whistle on the back of 汸 first, then 塡Write this page) i Cafe A6 B6 V. Description of the invention (iij 5-(4 monomethyl-1 pair of diazacyclohexyl)) 6 monofluoroazole methyl fluoride [1,5, m. P .in. 3 yl 1 > jy: i — tas — p — yl 5 — a) quinazoline, the hydrochloride (compound 37) decomposes at OOt, from 2 — ambience 4-(4 monomethylhexyl ) A 5_ trifluoromethyl oxazoline and 3 iso- radonyl methyl 1, 2, 4 — _ It is derived from cyclic propylene; hydrogen oxygenate is formed by dissolving alkali into the hydrogen gas of the methylene chloride. Ethyl 6-cyano-5-naphtholine-azoazole [1,5-a cool (compound 38), m.p. 196 in the preparation of gaseous diazepines and the addition of volatile] quinazoline-3 -1 9 8 It, a carboxylic acid is prepared by the reaction of 2-fluoro-5-fluoro-4-morpholine-oxazoline and iso- radonyl ethyl acetate; the base is 1, 2, 4-oxaziridine 1_ pair Diazahexyl)-6_trigasified methyl-a] oxazoline, hydrogen atmosphere (compound 39) 〇0t: decomposes at the time, from 2-atmosphere one group-1 pair of diazahexyl groups) A 5-trifluoromethyl-cyclopropyl- 3-isocyanatomethyl 1, 2, 4-3-(5-(azole m 5-cyclopropyl 4- monomethyl [1, 5 P .In 2 -3 -yl) _ 4-(4 -methyl-quinazoline and 5 m diazepines are prepared; hydrochloride is made by dissolving the alkali into the methylene chloride and adding gasification (please first Read the notes on the back of the page and fill out this page) The Central Standard of the Ministry of Economic Affairs is formed by printing and burning hydrogen in a consumer cooperative. 3 — (3 —Cyclopropyl 5-(trans-2, 5 — a) quinazoline (Compound 40 ) Based on 1, 2, 4-oxydiazepine S 5-dimethyl oxaline) a 6_ fluorine m. P. 4 1C, from 2-atmosphere-5-fluoro 4-(2, 5 -2 6-_ 5 _ group) -anilazole (1, 2 11-21 dimethylmorpholine) This paper scale is applicable to tfflS home «quasi (CNS) A 4 present grid (210 X 297 public S) 81.9.20.000 Printed by the Employee Consumer Cooperative of the Central Standards Bureau of the Ministry of Hydrocarbon Economy lioto A6 B6 V. Description of the invention (θ) — oxazoline and 3-cyclopropyl- 5 -isopropylmethyl — 1 t 2 »4 nitrogen dioxide «Compound 4 0 was prepared by column chromatography from compound 4 1> (eluent: methylidene nitride: ethyl acetate 1: 1))) 3 — (3 — cyclopropyl Group-1 > 2 »4 — gas diazo — 5 — group) — 5 — (cis — 2» 5 — dimethylmorpholine) — 6 — fluoro — quinazoline C 1 »5 — a] oxazoline (Compound 4 1) »m • P • 1 6 9 — 1 7 1» From 2 — atmosphere — 5 — fluorine — 4 — (2 5 — dimethylmorpholine) — oxazoline and 3 — cyclopropyl — 5 — isomylmethyl — 1 > 2 > 4 — prepared from oxydiazepine < compound 4 1 S Compound 4 0 was obtained by column chromatography 1 method Ί separation (eluent methylalide ethyl acetate (1 3 丄) () 5 * cyclopropyl — 1 »2 4 chlorodiazepine S — 5 — Group) — 5 a (N — (1 t 3 — dioxin — 2 — group) methyl — N monomethylamino group) — 6 — fluoro — zonazo rt 1 > 5 — a] quinazoline ( Compound 4 2) fm • P • 1 8 4 — 1 8 6 V > from 2 — atmosphere — 4 — (N — (1 > 3 — 二 m 院 — 2 — group) methyl — N — methylamine Radical) — 5 monofluoro-quinazoline and 5-cyclopropyl-3 — isocyanomethyl — 1 »pi > 4 — prepared from oxydiazepine S> 3 — (3 monocyclopropyl-1 > 2 9 4 — gas diazo m — 5 — yl) mono 5 -1 (cis — 2 »6 — dimethyl — 1 — pyridyl) — 6 — fluoro — mesoazole 1 I 5 — a] quinazole Porphyrin (compound 4 3) m • P • 1 3 2 — 1 3 4 * from 2 one gas one 4 one (cis one 2 * 6 — dimethyl one -27- ------------- - ---------- installed ------, ΓΓ ------ line (know first read the notes on the back of the clean page and then write this page) wood paper ruler general trapped Xijiabei Zhun (CNS) A 4 present lattice (210 X 297 g; $) 81.9.20.000 V. Description of the invention () 4) A6 B6 1 monopyridyl) 5-fluoro-oxazoline and 3-ring Propyl-5-isoradonylmethyl 1, 2, 4_ gas two ms prepared; 3 — (3 — cyclopropyl 1, 2, 4 — gas diazo S—5—yl) one 5-(3, 3-dimethylmorpholinyl) -6-fluoroquinazoline [1, 5 a ° C, consisting of quinazoline 3, 3 quinazoline 2-ambient and 3- (compound 44), m. p. 2 (3, '3-dimethylmorpholine 4 4-2 4 6)-5 _ gas-cyclopropyl- 5 -iso- radonyl methyl 1, 2, 4-gas-4-di It is prepared by Qimao; (please read the notes on the back of Qizhi first, and then write the clothes page). -Cyclone and palladium 3 6 -gas-yl) oxazoline 3 -ring N-(-quinazol [1, 17 0-17 dimethylaminopropylpropyl 5-isopropyl-1, 2 , 4_mdifluoros 2 -dimethylaminoethyl) -N- [1, 5-a] quinazole (Combined 2t, composed of 2-amino-6-ethyl) -N-ethylaminoaminomethyl-1, 2,4--5_ group) monoethylamino) one substance 4 5), m cyanide -4-(N) -quinazoline and nitrodiazepines-3-(3-cyclopropyl-1, 2, 4 -gas diazepines 5-4, 5-dihydrogen 5-oxo squint Azole [1, 5-a] quinoline 6-atmosphere 3-(3-cyclopropyl-1 1> 2 4 oxydiazepine_5-yl)-5 -morpholine quinazole [1, 5-a 〕 A quinazoline (1. 45g) dissolved in 25ml of 6MM amic acid at 45K: mixed for 45 minutes, and then the mixture in a cold aqueous solution, but to 0 t: and over 28- This paper ruler and applicable China Four standard (CNS) A4 specifications (210 X 297 g; $) 81.9.20,000 Α6 Β6 V. Description of the invention (〗 Γ) Filter out the sediment > 2 5 m! Of water and 5 X 1 m 1 of ethyl acetate > finally washed with 10 m 1 of diethyl m > dried crystalline product > available title of 8 5 S ί dagger compound tm • P-2 7 0 — 2 7 2 V (decomposition) 〇 Prepare the following chemical in a similar manner Compound 3 — (5 — Cyclopropyl- 1 > 2 · > 4 monochlorodiazepine-2-yl)-6-fluoro-4 5 monodihydro- 5-gas-zonazo r 1 »5 — A] Leptozoline »m • P • 2 6 〇— 2 6 4 V (decomposed) by hydrolysis of 3 mono (5 — cyclopropyl — 1 f 2 1 4 oxodim — 3 monoyl) 6 — fluorine — 5 — (3 5 dimethylmorpholine) benzozole — r L 1 »5 aj quinazoline to get 1 3 — (5 — cyclopropyl — 1» 2 »4 — m diaza δ — 3 — Base) — 7 — gas — 4 5 — 2 — M 2 — 5 — gas — zonazo C 1 > 5 — a oxazoline »m P • 〇5 4 — 2 5 5 ♦ By hydrolysis 3 — (5 — ring Propyl 1 1 2 2 4 4 — Chlorodirym — 3 — yl) — 7 Monofluoro — 5 — (3 »2 dimethylmorpholine) Myrazole—— [1 t 5 1 a J Quinazoline And -------------------------- installed ------. 玎 ------ line < know first ^ back Zhi; ± Nianshi-'; * Hori Script 1) Printed by MS Industrial and Consumer Cooperatives, Central Bureau of Standards, Ministry of Tobacco and Economic Affairs ¾ Obtained; Example 4 5, 6-two gas one 3- (3-cyclopropyl one 1, 2, 4, 4- oxo two gas one five-yl) one azole [1, 5_a] quinazoline-IS mixing The mixture contains 6-atmosphere-3-(3-cyclopropyl-1, 2, 4-oxydikryl- 5-yl)-4, 5-dihydro-5-1-oxazolidine [1, 5 — A] Quinazoline (1. Og), tripropyl-29- This paper scale i4 uses the Chinese and Western Standards (CNS) A 4 present grid (210 X 297 public goods) 81.9.20,000 ΙΑιή ,. Α6 Β6 The Ministry of Economy, Central Standards Bureau, g-consumer cooperatives printed 5th generation V. Description of invention) Amine (〇 • 5 m 1) and oxygenation m (5 m 1) »Heated under 1 4 〇 一 1 5 0 〇1 After hours »Add P 0 C 1 2 (5 m 1) and tripropylamine (0 * 5 m 1)» and heat for 1 * 5 hours 9 and then pour this warm mixture into 2 0 0 m 1 in water 9 and vigorously mix 〇1 after 5 minutes > add 1 0 〇m 1 of dimethane > collect insoluble substances in the water »wash with diacetic acid 9 After drying, the title compound can be obtained after drying» its It is a yellow-brown crystal 〇m • P * 2 3 8-2 4 〇 »Yield 0 • 4 7 〇 prepared by the method like a cocoon. Prepare the following compound 5-atmosphere-3-(5-cyclopropyl-1 > 2 * 4 — Myristadi-3-yl) — 6 — m — myrazole C 1 »5 — a] — quinazoline» from 3 — (5 — cyclopropyl-1, 2 »4 diazo Mao-3-base)-6 — Gas — 4 > 5 — dihydro — 5 — gas-triazole C 1 »5 — a J quinazoline, 5 — atmosphere — 3 one (5 — cyclopropyl-1 > 2 > 4 — gas diazo S — 3 monoyl) — 7 — fluoro-zole [1 * 5 — a] — quinazoline »m» P * 2 4 9 — 2 5 1 t > from 〇 — (5 — Cyclopropyl — 1 y 2> 4 — oxydiazepine — 3 — yl) — 7 — fluoro — 4, 5 — dioxo — 5 — oxypyridazole Γ 1 9 5 — a 3 quinazoline Obtained Example 5 (R)-6-m-3-(3-cyclopropyl-1 > 2 t 4-m Dihemo-5-yl)-5-(2 monohydroxymethyl-1-at Alkyl) — quinazoline C 1 »5 a a quinazoline (compound 4 6) -30- (please read the notes on the back before writing a wooden page) This paper size and degree are suitable for Chinese and Western Jiafen Standard (CNS) Ψ 4 present grid (210 X 297 g: S) 81.9.20.000 A6 B6 V. Description of invention U1 ")) A mixture, including mg) and triethylamine 9), which is based on droplets (3-ring 1, 5 F (5 m filter anti-sleep mixed for 10 minutes to obtain the title 2 2 1 V with a similar 6 _ gas--group)-propyl one 1, —a〕 —quino 1) Suspension, leaching solution. After leaching the compound, its production is 0. Method of preparing 3- (3- 5 -thiomorphate 4 7), m · p (R) 2-hydroxymethylpyrrolidine (70 0 mg) Dissolved in anhydrous DMF (1ml added to a solution containing 5, 6-two atmospheres 3-2, 4-gas diazenium-5-yl)-zazolazoline (0.20s) dissolved in anhydrous DM liquid, ' The temperature is Ot :. After 20 minutes, the resulting crystalline product was diluted with 15 ml of water and mixed under Ot :, washed with water, and dried to become yellow crystals. m. p. 22 Ο-Ι 5 g. List of compounds: Cyclopropyl 1, 2, 4-gas two gas S_5 oxazoline [1, 5-a] oxazoline (Chem. 24 0-241C, from 5, 6-di atmosphere-3-) Anilazole 6 —Gas_ (3 —Cyclopropyl_1,2, 4 —Oxydioxolane-5-yl, 5 3- (3- ---------------- -------- Installed ------, ΤΓ ------ line (read the notes on the back of 汸 first, then fill out this page> a) Quinazoline and thiomorpholine Separately prepared by the Ministry of Economic Affairs Central Standards Bureau tH Industrial and Consumer Cooperatives Co., Ltd. Cyclopropyl-1, 2, 1-yl) -5— (cis-2,6-dimethyla) quinoline (Compound 48), m , 5 4 one gas two gas S porphyrinyl) -mizole. P. 2 3 6 -5 2 3 8, prepared from 5, 6-mit rr pent-death-6 dimethylmorpholine; 4 _ gas Bis-cis 2, bis-gas 3 — (3-cyclopropyl_1,2, yl) -quinazoline [1, 5 — a] quinazoline and (S) 6 — gas — 3 — (3 — ring Propyl 1,2,4 3 1 The scale of wood paper is in accordance with the Chinese and Western standards (CNS> A4 specifications (210 X 297 public goods). Oxygen 81.9.20,000 Printed by the Ministry of Economic Affairs Zhongjiabei Zhugongju Industrial Co., Ltd.% A6 B6 V. Description of the invention (Μ) Nitrogen-5-yl) -5 2 —Methylmethyl_1_pyrrolidine) quinazoline [1,5_a] quinazoline (Compound 49), mp 266 — 269 ° C, consisting of 5, 6 — diazo 3_ (3 — cyclopropane Based on 1,2,4-oxodioxamonoyl) monozole [1,5-a] quinazoline and (S) _2 —methoxymethylpyrrolidine; (S)-6 — 3-1-3 (3-cyclopropyl-1, 2, 4-oxodimethan-5-yl) -5- (2-rea-ylmethyl-1- (ft taryl)) benzoazole [1 . 5-a] Quinazoline (compound 50), m.P. 230 — 232t, consisting of 5, 6-dichloro- (3-cyclopropyl-1, 2, 4_ oxydioxa-5-yl) Li [1, 5-a] quinazoline and (s)-2-hydroxymethyl at pyrrolidine prepared; 6-m-3-(3_ cyclopropyl 1, 2, 4-chlorodicyanide Molo-5 yl) -5— (3-hydroxy-1-1-shodinyl) quinazoline [1, 5-a] quinazoline (compound 51), m.P. 258-261 from 5, 6-di Gas 3 — (3_photopropyl-1, 2, 4, — «diazepine-5-yl) -quinazole [1, 5—a] oxazoline and 3-hydroxy help pyridine prepared; 6— Chlorine-3 — (3-cyclopropyl one 1, 2, 4-chlorodiazepine S-5 monoyl) —5- (4-phenyl-1 1 pair of diazahexyl ring) -squinazole [1,5-a] siazolin (Compound 52), m. ρ · 255-2 57t :, from 5, 6-dihydrogen 3 — (3- cyclopropyl 1, 2, 4-gas diazonium S — 5 — yl) monoazole [1, 5 — a] Prepared by quinazoline and 1-phenyl-p-diazepine; -32-. The paper scale is applicable to the Chinese standard (CNS> A 4 present grid (210 X 297 mm) 81.9.20.000- ----------------------- installed ------ tr ------ line (please read the notes on the back of 汸 before filling in (This page)

C.M A6

Printed by the Central Standards Ministry of Economic Affairs, Consumer Cooperatives, and the Fifth, Invention Note 1) 6 — Atmosphere 3 — (3 — Cyclopropyl 1, 2, 4 — oxydiazepine S-5 — base) _5 — ( 4 monomethyl-1 1 pair of diazacyclo) -imidazole [1,5-a] quinazoline (compound 53), m.P. 273-2 7 2 t :, from 5, 6-dihydrogen 3-(3-cyclopropyl-1,2,4-nitrogenazo-5--yl) -quinazoline [1, 5-a] quinazoline and 1-methyl-p-diazepine are prepared; 6 —Gas 3 — (3 —Cyclopropyl—1, 2, 4 —Gas dichloromethane—5 monoyl) —5_ (4 — (2-hydroxyethyl) —1 pair of diazahexyl)- Pyrazole [1, 5-a] Leptozoline (Compound 54), m.P. 252-254X :, from 5, 6-diamine-3-(3-cyclopropyl-1, 2, 4--gas Diazono-5-yl) -quinazoline [1,5-a] quinazoline and 1- (2-hydroxyethyl) -p-diazepine; prepared from 5-amino-6-ambient-3 — (3-cyclopropyl-1, 2, 4-oxodiazepine S-5-yl) quinazoline [1, 5-a] quinazoline (compound 55), m.p. 343T ;, by 5 , 6 — two gas one 3 — 3 Monocyclopropyl-1, 2, 4-gas diazenium-5-yl) quinazoline C1, 5_a] quinazoline and ammonium aqueous solution are prepared by cracking; 6 —gas 3_ (3 — cyclopropyl-1 , 2,4 one gas two S-5 monoyl) 5_ (4-propyl-1-pyrazine ring) _ 眯 azole [1, 5-a] #zoline (compound 56), m. P. 186-188t :, consisting of 5, 6-difluoro-3- (3-cyclopropyl-1, 2, 2, 4-dinitrogeno-5-yl) -quinazoline [1.5-a] quinazoline -3 3- This paper ruler 71 universal taa standard (CNS) A 4 specifications (210 X 297 male; $) 81.9.20.000 .........- Ι1ΓΙΙ I-.-«. ' .'βτι, ι,. I, I .ϋ ^ ΐ || Ι || Ι · Ι | ΙΜ | ί · 〇αlν-4 * 1 · > ·) ί9 ** > ι '[ηΐϋ (II « · »· '&Quot; *-. ..... \ * β ulltl λ« -ι ·-·' —a 外 — < ------------------ ------ Pretend ------ tr ------ Marry (please read the note on the back of the 汸 first and then write this page) 〆 / 9 ·, ^ ΙΧύΌό Α6 Β6 V. Invention Explanatory Note: The employee consumer cooperative of the China Bureau of Standards, Ministry of Economic Affairs, prints «and a 1-propyl p-diazepine prepared from i 3 — (5 — cyclopropyl — 1 & g t; 2 »4 oxodiazin-3-yl)-6-fluoro-5-morpholinyl-zonazo r 1» 5-a quinazoline (compound 2 1) »m • P • 2 0 4 — 2 0 6, consisting of 5 — gas — 3 — (5 cyclopropyl — 1 2 f 4 — m diazepine — 3 monoyl) — 6 monofluoro — zonazo C 1 > 5 — a] ® · oxazoline and Preparation of morpholine yields t 5 — (N — cyclopropylmethyl — Ν — methylamino) — 3 — (5 — cyclopropyl — 1 »2 series 4 — gas diazide — 3 — group) — rn — Fluorine-Fenazole [1 > 5 a, a] Quinazoline (compound 5 7) »m • P • 1 7 6 — 1 7 7 t: > from 5 — nitrogen — 3 — (5 — cyclopropyl Radical 1 »2 > 4 — gas diazonium S — 3 — yl) — 7 — Μ — benzozole C 1» 5 — a] quinazoline and (N-methylaminomethyl) cyclopropane To get t 3 — (5 — cyclopropyl — 1 »2 * 4 — gas two gas S — 3 — 1) — 7 — fluoro — 5 — (3 — m oxazolyl) — zonazo [1 9 5 1a> Quinazoline (Synthetic Compound 5 8) * m-P • 2 4 0 — 2 4 2 t: > from 5 — atmosphere — 3 — (5 — cyclopropyl — 1 > 2 1 4 — oxodiane m — 3 monoyl) — 7 monofluoro-imidazole Γ 1 1 5 — a] quinazoline and thiazole prepared from * 3 — (5 monocyclopropyl — 1 t 2 t 4 — oxydiazepine — 3 — Radical) — 7 — fluoro — 5 — morpholine — myrazole C 1 t 5 — a quinazoline (compound 5 9) »m • P • 2 1 3 — 2 1 4 t: > from 7 — fluoro — 3 One (5 — cyclopropyl — 1 > 2 > 4 — m dikryptomene — 3 — yl) — 5 is prepared from an oxazolidine C 1 * 5 — a] m oxazoline and morpholine to give i- 34- The size and degree of this paper are applicable to the standards of the middle and poor countries (CNS > A4 present grid (210 X 297 g; S) 81.9.20,000 ------------------- ----- Pretend ------ ir ------ marry < Please read the back of the 汸 first; ± read the matter and then write this page) ZTE Standardization Bureau of the Ministry of Economic Affairs 3Work Consumer Yin Fen ^ X JL 0 ^ Α6 _Β6_ V. Description of the invention (i 丨) 3-(5 —cyclopropyl 1, 2, 4 — oxydiazepine S — 3 —yl)-5-(1, 3 -dioxane- 2 -spiro-4′-pyridinyl)-7 -fluoro-pyrazole [1, 5- a] Quinazoline (compound 60), m.p. 245-246¾, consisting of 5-ambient 3- (5-cyclopropyl-1,2,4-pyridine-3-yl) -7-fluoro Yiweili [1, 5-a] quinazoline and 1, 3-dioxane- 2 —spiro-4 ′-# prepared from pyridine; 3 — (5 — cyclopropyl_1, 2, 4 — oxygen Diazo S 3 -yl)-5-(N — (2-dimethylaminoethyl) -N-methylamino) -7-fluoro-quinazol [1, 5-a] oxazoline (Compound 6 1), m.p. 148 — 150 ^, consisting of 5-Amino 3-(5 -cyclopropyl 1, 2, 4-oxydiazepine S 3 -yl)-7-Fluorine Azole [1,5—a] Leptazoline and N, N, Ν′-dimethylethylenediamine are prepared by cracking; 3-(5-cyclopropyl-1, 2, 4-oxodiazepine-3 — Group) — 6-fluoro-5- (4-methyl-1-p-diazepine) quinazoline [1, 5-a] quinazoline (compound 62), m. P. 2 7 4 -276 ^, from 5 — atmosphere one 3 — (5 —cyclopropyl one 1, 2, 4 — gas di ms — 3 —yl) —6-fluorofluoroquinazoline [1, 5-a] quinazoline and 1_methyl-p-diazepine are prepared; 3 — (5-cyclopropane A 1,2, 4-gas diazepine-3-yl)-6-fluoro-5-(4 one (2- hydroxyethyl)-1 a pair of diazohexyl)-azoazole [1, 5 — A] Quinazoline (compound 63), m. -35- (please read the notes on the back of 汸 before writing this page) • Installation · Order-• Line. This paper ruler is applicable to 囀 囲 a house standard (CNS > A 4 present grid (210 X 297 public 3E) 81.9.20,000 Employee consumption cooperation of the Central Bureau of Economics and Politics for printing and burning 2 ϋ〇υ〇Α6 Β6 V. Description of invention (U) P 2 2 8 — 2 3 〇t : ≫ from 5 — nitrogen 3 — (5 monocyclopropyl — 1 »2 > 4 — oxydiazepine m — 3 — yl) 6 — fluoro — zonazo r L 1 > 5 — aj quinazoline And 1 — (2 monohydroxyethyl) p-diazepine ring to prepare «3 — (5 — cyclopropyl — 1 > 2» 4 — oxydiazepine S — 3 — yl) — 7 — fluorine — 5 — (N — (2 hydroxy Group) — N — methylamino group) — zonazole C 1 »5 — a] quinazoline (compound 6 4)» m • P • 1 6 1 — 1 6 3 X: > from 5 — atmosphere — 3 One (5 — cyclopropyl — 1 > 2 • 4 — m diazo — 3 — group) — 7 — gas — imidazole C 1 »5 — a J quinazoline and — (N-methylamino) ethanol Prepared to give 2- (5-cyclopropyl-1> 2 4 — chlorodi S — 3 — yl) — 7 — cyano — 5 — (4-m piperidinyl) — quinazole C 1) 5 — a Ί quinazoline (compound 6 5) »m • P • 2 3 4 — 2 6 1C (decomposition) * from 5 — atmosphere — 3 — (5 — cyclopropyl-1 1> 2» 4 — oxydioxa 3 — yl) — 7 — fluoro-imidazole r 1 * 5 — a] Quinazoline and 4-pyridone are prepared by cracking to obtain 3 — (5 — m propyl — 1 > 2 t 4 — chlorodiazepine — 3 — yl) — 7 one gas — 5 — (N — methyl — N — 1 — methyl-4-pyridyl) amine) — zonazo r 1 f 5 — a 3 quino Porphyrin (compound 6 6) > m P • 2 0 4 — 2 0 7 »from 5 — atmosphere — 3 one (5 — cyclopropyl — 1 > 2 > 4 mononitrogen — 3 — group) — 7 1-fluoro-zirconium 1 > 5-a] Quinazoline and 1-methyl-4-((methylamino) pyridine prepared from 1-36- ------------ ------------ installed ------. 丌 ------ ^ (Please read the notes on the back of i $ before writing this page) This paper size is applicable Western Standard (CNS) A 4 Said (210 X 297 g: ¾) 81.9.20,000 Printing and Burning Αβ _B6_ of the Consumers ’Bureau of the Ministry of Economic Affairs of the Ministry of Economic Affairs Αβ _B6_ V. Description of Invention (Μ) Example 6 5_Morpholine 1 [2,5-a] quinazoline 3_carboxaldehyde amine «mixed mixture, including ethyl 5-morpholine-triazole [1, 5 a] oxazoline 3-carboxylic acid Ester (2.0 g) and ethyiamine (1.2 g) were dissolved in 20 ml of anhydrous dimethylformamide, heated at 80 t: added 30% dissolved in methanol (1 m 1) The solution of sodium methoxide and fusidium was mixed with this mixture for 2 hours at a temperature of 100t. Cool to room temperature and dilute with isopropanol (20ml). After leaching out the crystals, rinse with isopropanol (15ml), water (20ml) and diethyl ether (10ml). After drying, you can obtain the title of yellow crystal The compound, m.p.> 300 ^ 0, yield 1. 3g. Example 7 3-m-based 5- 5-chrysoline-monozole [1,5-a] quinazoline (combined 拗 6 7) in the form of droplets of desert (0.15ml) added to a triphenyl-containing compound ( 0. 8 g) dissolved in a solution of 15 m 丨 methylene chloride, the temperature is to be a porphyrin-zonazo [1, 5-a] #zoline-3-carboxamide (0.5g) and Triethylamine (0.83 mi) was added to this solution, and the results were mixed at room temperature for 3 hours, and then evaporated in the air. Ethyl acetate (10 m 1) was added to the residue, and then the crude crystals were separated by filtration. The dried crystalline material was dissolved in acetone (30 ml), and an excess of hydrogenated atmosphere dissolved in diethyl ether was added to separate the argon chlorinated compound of the title compound, which was a crystal of beige. Μ -3 7- This paper ruler and the common standard (CNS) A4 specifications (210 X 297 public goods) 81.9.20,000 ------------------ ------ install ------. 玎 ------ ^ (please read first-the notes on the back and then write this page) A6

5. Description of the invention (W) {Sait first read the notes on the back and then write the clothing page). Ρ · 225-223t, yield 0.3g. Prepare the following compounds in a similar manner: 3- radon-8-methoxy-5-morpholinyl-quinazoline [1,5-a] quinazoline (compound 68), m.p. 283-284 r, Derived from the cracking of methoxy-5-mazoline quinazoline [1, 5-a] oxazoline 3_carboxy. Aldamine. Example 8 5-Morpholine quinazoline [1, 5_a] quinazoline -3-carboxamide oxime a mixture, including sodium gas vapor (0.06g), hydroxylamine radium odorate (0.10g) and Methanol (3ml), which was stirred at room temperature for 1 hour. The reason is that the hydroxylamine is separated by filtration. It is a formazan solution. The filter cake is washed with methanol (7m 丨). Hydroxylamine solution was added to a suspension containing 3-cyano-5-morpholine monozole [1,5-a] quinazoline (0.16 g) dissolved in 5 ml of methanol. The reaction mixture was flowed for 4 hours, cooled to room temperature and filtered. The crystalline product was rinsed with methanol and dried to give the title compound as yellow crystals, m.p. 212-213TC, yield 0.17g. Spring Example 9 Central Standard Wu S Industry and Consumer Cooperative of the Ministry of Economic Affairs of the Republic of India 5th generation 5-morpholine 3- (5-tricyanomethyl-1, 2,4 oxydiazepine-3-yl) -pyrazole [1, 5-a] Pyrazoline (Compound 69) Trifluoroacetic acid (0.15 ml) was added in the form of droplets to a mixture containing 5-morpholine-quinazoline [1, 5-a] quinazoline_3_carboxy Amidoxime is dissolved in a suspension of 4m1 of anhydrous tetrahydrofuran and stirred at room temperature for 3 -38 " 81.9.20,000. The paper size is applicable + National Standards (CNS > almost 4 grids (210 X 297 mm) A6 B6 η »^ V. Description of the invention (5Γ) (Please read the notes on the back before writing this page) Hun Jun, evaporate the reaction mixture in the air. Dissolve the residue in the mixture of water and ethyl acetate Medium. The organic phase layer was washed with water, dried over anhydrous magnesium sulfate and evaporated to dryness. The crystal S was mixed with isopropanol (3ml) and washed to give a yellow title crystalline compound, mp 182-18 Yield 0.06g. Example 1 0 3-(5-Cyclopropyl 1, 2, 4-gas diazenium 3-yl)-6-methoxy-5-morpholine-azole [1, 5 — A〕 Quinazole (Compound 70) A mixture containing 6-methoxy-5-morpholine-imidazole [1.5-a] quinazoline-3-carboxylamide oxime (0.9g), ethylcyclopropyl Carboxylic acid ester (1.7 g), molecular sieve (3 g), and 80% Mn (0.1 g) were dissolved in 20 ml of anhydrous DMF, which was heated at 120 t for 1.5 hours, and the mixture was cooled to At room temperature, dilute barley (20 ml) with acetic acid (0.5 ml) and formazan, and filter it. The filtered mixture was evaporated and purified by column chromatography (HPLC) (eluent: A Supporting compound: acetone (2: 1)), the title compound can be obtained as yellow crystals, mp 227-228t, the production and consumption rate of the Employees ’Cooperative of the Central Bureau of Standards and Economics, 0.38 g. The following method is prepared in a similar manner Compound = 3 — (5 — (1 —methylcyclopropyl) — 1, 2, 4 — gas diazenium-3-yl) — 5 — morpholine quinazoline [1, 5-a] quinazoline ( Compound 71). M. P. 232-236 It is composed of 5-morpholine-39- 81.9.20.000. The paper size is applicable to the national standard (CNS) sub 4 specifications (210 X 297 public goods) U such as A6 _B6_ Fifth, the description of the invention (砘) Face to face: iis matter and then write this page) Izozole [1,5-a] € oxazoline 3-carboxylamide oxime and ethyl 1-methylcyclopropyl carboxylate are prepared. Examples 1 1 3-(3-cyclopropyl-1, 2, 4-chlorodiazino-5-yl)-5-(1-oxo-thiomorpholine) monoimidazole [1, 5-a] quinazol (Compound 7 2) and 3- (3-cyclopropyl-1, 2, 4_m diazenium-5-yl)-5-(1-dioxathiothiophenoline) -mazole [1, 5-a 〕 Oxamorphine (compound 7 3) a solution containing 3- (3-cyclopropyl 1, 2, 4-gas diazo S-5-yl)-5-thiomorpholine-myrazole [1 , 5 — a] Quinazoline (0.5g) and 30% aqueous solution (0.2 ml) of over-aerosolized radium were dissolved in 15ml of acetic acid, and it was allowed to flow for 40 minutes. After cooling to room temperature, filter out 3- (3-cyclopropyl-1,2,4-gas diazo S-5-yl) -5- (1,1-dioxo-thiomorpholine)- The crude crystalline product of quinazoline [1, 5-a] quinazoline can be recrystallized from DMF to obtain a pure product, M.P. 328-335f, with a yield of 64 mg. Printed by the Ministry of Economic Affairs Central Standard Industry and Consumer Cooperative Society « The acetic acid that has passed through evaporates in the air, and the residue is mixed with water (10 ml) and filtered to obtain 3- (3-cyclopropyl-1,2-4-oxo-SS-5-yl) _5-(1 1oxy-thiomorpholine) _ quinazoline [1,5-a] quinazoline crystal crude product, recrystallized from DMF to obtain a pure compound, M. p. 293-294t :, yield 0.2s . -40- 81.9.20.000 The size of this paper is universal t Guo Xijia standard (CNS> Yu 4 present grid (210 X 297 mm) "For example, A6 ^ _ V. Description of invention (彳 q) Matters needing attention and then fill out this page) 霣 例 1 2 7 — Fluoro-3-(3-Isopropyl 1, 2, 4-Oxygen Dioxide S-5 Monoyl)-5-Morpholine-Mizole [1 , 5-a] Quinazoline (Compound 7 4) A mixture containing ethyl 7-fluoro-5-morpholine-quinazoline [1,5-a] quinazoline-3-dwarf acid ester (1 6g). 2-Methyl-1-propane carboxylamine oxime (2.4g), crushed 4A molecular sieve (3.5g), and sodium hydride (0.14g, 80% dissolved in mineral oil ) Dissolve in 20ml of anhydrous DMF and mix at room temperature. After one hour of dredging, add carboxyl oxime (2.4 g) and sodium hydride suspension (0.1 4 g). The mixture was added for 1 hour, and glacial acetic acid (2ml) and dichloromethane (50ml) were added. After the sediment was dissolved. The molecular sieve was filtered through diatomite. The filtrate was evaporated, and the residue was ground with 100m1 of water, and the undissolved part was collected by filtration. Portion, dried and treated with 25 ml of acetone. The yellow crystalline product is obtained and the Drying, yield 0.47g, m.p. 262-264t: 〇Printing and Burning-41 of the Central Bureau of Standards of the Ministry of Economic Affairs, WK Industrial and Consumer Cooperatives-41- This paper ruler and the general trapped a home standard (CNS) A 4 specifications < 210 X 297 public: $) 81.9.20,000

Claims (1)

6. Patent application scope A7 B7 C7 Γ: D7 f:.-An imidazoline compound of formula I And pharmaceutically acceptable acid addition salts or hydrates, where Q is 〇-? F ίί-0 // ο ~ ιτ Μ-Ο (Please read the notes on the back before writing this page) -C.QOR8 or -CN; where R1 is hydrogen, straight or branched alkyl, unsubstituted or C! _S alkyl substituted C3 _7 cycloalkyl, Ci alkane, C! Alkane One Ci _s _ alkyl group or triargyl methyl group; R8 is the Ministry of Economic Affairs of the Ministry of Economic Affairs KC Gongxiao &<; K He Yi She printed ー I C-3 Institute Chlorine instead of RS Alkanes and II Or sex group ζ 1 e group selected benzene RCI alkane-or, 1 S-group, the group C _ aminoamino alkane, 1 alkyl pyridyl group CS alkane oxane | 1 I of the se group 1 S generation-i Esteryl C | Take 1 1 methane, 1 group c C, lffic alkane, one group 6 is an e group alkyl group I other two I alkoxy one point, 1 squalane SC 2 group c 7 s I R alkane With |-slit and ring 3 1C branch 2.1 sex c CI or R 7 is selected, the base S other group carbonyl straight η or gas distribution basic Jiu Youjia (CNS) A · ί HA (2U) X Second, the father ), F \ Six, the scope of patent application ring or non-cyclic copper condensate, or R2 and R3 and the nitrogen atom to form a 4-6 6 atom cyclic amine group, in the ring system, one or more tilted atoms Can be exchanged with nitrogen, gas, sulfur, sulfinyl, sulfonyl or carbonyl, or its hydrate , A non-cyclic or cyclic ketal, each value of these ring systems can be selectively one or more values Ci _6 alkyl, Ci _6 alkoxy monomethyl, hydroxy, Ci + S-hydroxyalkyl Or substituted by phenyl. R 4, R 5, Rs are hydrogen, hydroxy, Cl, Br, F, I, trifluoromethyl, nitro, amine, nitrogen, straight or branched C! _ S alkyl, c2 alkenyl , C2 _6 -alkynyl group, Ci _6 yard gas group, C 1 _ S @ 气 基 _〇1 _ s yard group or C 1 _ s-yard gas group carbonyl group; the restriction is that when Q is (Poetry first reading « (Notes on the back will write this page again) Central Ministry of Hydrocarbon Economy M: Work Consumers «· Cooperative Society Seal 5; Ring I Generation 5 7 3 Take an I cg nitrogen 3, not | C base a 6 chloro-based hydrogen alkyl form B is taken i 3 Yes It can pass e R but not without I eg or -R contract group c N 7 alkane 丨,: | or 1 R 6 Η basic formula, I is alkane 6 1 different I and RW points S 'I 3 | 5 HR 1? R is with C generation, 2 or sulfur 4 1 R group or RR., Alkanoline, in the middle of the ring is its alkane 7 (CN?) Τ7 4 CIO X:; · 7 ν) ATb3 B7 C7 D7 Six. The scope of patent application-morpholine-triazole [1,5-a] oxazoline 3-carboxylate or 6 atmosphere of 3- (3-cyclopropyl-1,2,4-pyrazole A 5-base) 5-morpholine-domain azole [1, 5-a] azole. 2. If the compound of item 1 of the patent application scope, where Q is enthalpy &gt; ro (Poetry first read the notes on the back of tr and then write this page) Economical Central Bureau of Standards to: work; fl fee cooperation to make prints — C0'0R8, or CN, RL is Jingpropyl, methyl Cyclopropyl, isopropyl, methylmethyl or trifluoromethyl, R8 is ethyl, isopropyl or tert-butyl, and its pharmaceutically acceptable Xue addition salts or hydrates. 3. Compounds as claimed in item 1 or 2 of the patent scope, where R 2 and RA are hydrogen, methyl, ethyl, hydroxyethyl, methylchloroethyl, 2,2-dimethylaminoethyl , Dimethylaminoethyl, cyclopropylmethyl, ethoxycarbonylmethyl, N-methylpyridinyl or (1, 3_dioxane-2-yl) -methyl, or R2 and R3-together with the nitrogen atom to form chrysoline, thiomorpholine, gas mono- or dichlorothiomorpholine, K-pyrrolidinyl, pyridinyl or thiazolidinyl, each of these ring strips is selected Propyl, propyl, phenyl, hydroxy, hydroxymethyl, hydroxyethyl or methoxymethyl substituted, and its pharmaceutically acceptable acid addition g or hydrate. 4. The compound as claimed in item 1 of the patent scope, wherein R4, R5, R6 and R7 are hydrogen, C1, Br, F, 0 C Η 3. C Ν, trifluoride methyl or methyl (CNS) r 4, ·:! 0 X: r- ~) i: A7 B7 C7 D7 VI. Patent scope or hydrate. 5. If the compound of the first item in the scope of patent application, it is also from: 3-(3-propyl propyl 1, 2, 4-gas diazenium-5-yl)-7-krypton-5-morpholine one Imidazole [1, 5-a] quinazol, 3-(3-cyclopropyl-1, 2, 4, oxydiazepine-5-yl)-5-morpholine 6-trifluoromethyl squint Azole [1, 5_a] quinazoline »3-(3-Jing propyl 1,2, 4-chlorodiazepine S-5-yl)-6-Qi Yi 5-Mom told a sleep [1 # 5 — A] Quinazoline, 3 — (3-cyclopropyl—1,2,4-chlorodiazepine S — 5 —yl) — 6-fluoro-5- (cis-2,6-dimethylmorpholine) Azole [1, 5-a] Ozarin, 3-· &lt; 3-Cyclopropyl-1, 2, 4 -gas diazenium-5-yl) -6-fluoro-5-thiothio _ 眯 陛 〔1, 5-a〕 Quan, 3 1- (3-cyclopropyl-1, 2, 4-oxodiazepine-5-yl) mono-6-fluoro-5- (4-monomethyl Yl-1-p-diazepine (yl) -pyrazole [1, 5-a] quinazol, 3-(5-cyclopropyl 1, 2, 4-oxydichloromethane-3-yl)-5 — (Anti-2, 5 — two Ylmorpholine) -6-gas-imidazole [1,5-a] quinazol 3- (5-cyclopropyl-1,2,4-oxodiohydra-3-yl) -5- (cis-2, 5 — dimethyl?) 6—® — 眯 _ [1, 5 — a] Quinazol, (please read the notes on the back first and then write this page) ·-* -Driver · Economic Central Government Bureau of Standards w: printed by industrial and consumer cooperatives * A7 B7 C7 D7 e Ministry of Economic Affairs Central Kneading Rod Bureau "two" &";" and "combination permit printing" "Six, apply for patent scope 3 one (3-cyclopropyl one 5 one m azole) one 6-fluorine one 5- Linimidazole C 1 9 5 — a] Quinazoline 9 3 mono (3 -cyclopropyl — 1 »2 9 4 — gas diazoxide mono 5 — yl) — 5 mono (N — (1 &gt; 3 — diox -2-yl) methyl-N-methylamino)-6-argon quinazoline C 1 »5-a 3 quinazoline» 3 one (5 — cyclopropyl — 1 I 2 »4 — gas Diazepine — 3 — yl) — 5 — (2 1 6 — dimethyl / 1 — pentidinyl) — 6 — fluoro — mebendazole C 1 &gt; 5 — a 3 m oxazoline 0 6 • one for The m-composition I for the treatment of m-neuropathy includes-quantitatively the compound as claimed in item 15 of the patent application or its pharmaceutically acceptable acid addition compound and a pharmaceutically acceptable halberd Rush or m release agent 〇 .7 • For example, the compound in the patent scope item 6-item «which is in the form of a p-dosage t t containing 0 • 1-1 〇〇mg active compound 〇8 • as the patent application item 1 compound Meng Qi is m in preparation-a scientific composition that is thrown to treat m in the planting of the sacred ridge system disease. QQ: If you want to benefit from the scope of the gth-eight_ &gt; its Ψ the disease is spasm mt Jiao Lu or Insomnia 〇1 0 A method for preparing a compound as claimed in any one of items 1 to 5 in Patent «w Surrounding, characterized by a) reacting a compound of formula II and a compound of formula III, (please read the notes on the back first Write this page again) This (CNS) γ (.2 '' X: Factory II, U) ό Α7 Β7 C7 D7 Patent application scope E _ (π) (Please read the precautions on the back before entering this page) where R2, R3, R4, RS, RS @ R7 are as defined in item 1 of the patent application scope, where Y is a leaving group, C Ν-C Η 2-Q (III) where Q is as defined in item 1 of the patent application, to form a compound of formula I, or b) reacting a compound with a general formula IV and a derivative The compound of formula V:-窣-• ^ · CCOH V). Comprehensive · Fe Ministry of Economics Central Bureau of Quotations w: Cooperatives & Cooperatives Cooperatives where R2, R3, R4, Rs, R6 and R7 are as defined in item 1 of the patent application scope, Rl-C (= NOH) NHz (V) where R1 is as defined in item 1 of the scope of the patent application II to form a formula -6-in this ruler? ; (CNS) A 4 (210 X 297 II, 9) A7 B7 C7 D7 VI. Patent application scope I compounds, where Q is Where R1 is as defined in item 1 of the patent application scope, or c) reacts a compound of formula VI and a dehydrating agent, (please read the note on the back of the leap before writing this page) 7 n XT Where -R2, R3, R4, Rs, Rs and R7 are as defined in Item 1 of the patent scope to form a compound of formula I, where R2, R3, R4, Rs, Rs and R7 are as applied Defined by patent scope • Jurisdiction. This ruler Λϋ Blade Middle (CNS) A 4 (210 X II, male) 6. Scope of patent application. · Among them, R 2, R 3, R 4, R 5, R 6 and R 7 are as defined in item 1 of the patent application scope to form a compound of formula VIII Where R2, R3, R4, Rs, Rs and R7 are as defined in item 1 of the patent application scope, and reflect this formula VI I Γ compound and R1-C〇OE t or and (R1 C0) 2 0 , Where R1 is as defined above to form a compound of formula I, where Q is (please read the precautions on the back before writing this page) N-0 Where R1 is as defined in item 1 of the patent application scope, or e) hydrolyze the compound of formula I to form a compound of formula I X Central Ministry of Economic Development, Ministry of Economic Affairs *: Gong &quot; &quot; Cooperative Society * X The original meaning is in use? : Automobile pregnancy (CNS) A 4 (210 X y male) • Α7 Β7 C7 D7 Six, the scope of patent application, Q, R 4, R 5, R 6 and R 7 is the first place in the application for “ϋ patent range” As defined in the item, and the compound of formula IX and POC 13 are reacted to form the compound of formula X X It reacts with the compound of formula X I N H R 2 R 3 (XI) where .R2 and R3 have the definition as defined in item 1 of the patent scope to form the compound of formula I. (Please read the precautions on the back before writing this page) This Approval A China Home (CNS) A 4 (21C X)